What are the common side effects of Labetalol HCl. How does Labetalol work in the body. What precautions should be taken when using Labetalol. Who should avoid taking Labetalol. How is Labetalol administered and dosed. What are the potential drug interactions with Labetalol. When should you seek medical attention while taking Labetalol.

Understanding Labetalol HCl: A Powerful Antihypertensive Medication

Labetalol HCl is a widely prescribed medication used to treat high blood pressure (hypertension). It belongs to a class of drugs known as alpha and beta-blockers, which work by affecting the response to certain nerve impulses in various parts of the body. This dual action helps reduce blood pressure by decreasing heart rate and relaxing blood vessels.

How does Labetalol work in the body?

Labetalol works by blocking both alpha and beta receptors in the body. By blocking beta receptors, it slows down the heart rate and reduces the force of heart contractions. Simultaneously, by blocking alpha receptors, it causes blood vessels to dilate, which reduces blood pressure. This combined effect makes Labetalol particularly effective in managing hypertension.

Common Side Effects of Labetalol HCl

While Labetalol is generally well-tolerated, like all medications, it can cause side effects. The incidence and severity of these side effects often depend on the dosage. Here are some of the most commonly reported side effects:

• Dizziness
• Fatigue
• Nausea
• Vomiting
• Dyspepsia (indigestion)
• Paresthesia (tingling sensation)
• Nasal stuffiness

It’s important to note that these side effects tend to increase with higher doses of Labetalol. For instance, at a daily dose of 200 mg, only 2% of patients reported dizziness, while at 2400 mg, this increased to 16% of patients.

Are there any serious side effects associated with Labetalol?

While less common, some serious side effects may occur with Labetalol use. These include:

• Symptomatic postural hypotension (a sudden drop in blood pressure when standing up)
• Ventricular arrhythmia (abnormal heart rhythm)
• Wheezing
• Increased blood urea nitrogen and serum creatinine levels (particularly in patients with prior renal insufficiency)

If you experience any of these serious side effects, it’s crucial to seek medical attention immediately.

Labetalol Administration and Dosage Considerations

Labetalol is available in various forms and strengths, including oral tablets and injectable solutions. The dosage and administration method depend on the patient’s condition, response to treatment, and other factors.

What are the available forms of Labetalol?

Labetalol comes in several forms and strengths:

• Oral tablets: 100 mg, 200 mg, and 300 mg
• Injectable solution for intravenous use

The tablets come in different colors and imprints to help identify the strength:

• 100 mg tablets are typically yellow or beige
• 200 mg tablets are usually white
• 300 mg tablets are often green or blue

How is the dosage determined for Labetalol?

The dosage of Labetalol is individualized based on the patient’s response and the severity of their condition. Generally, treatment starts with a lower dose and is gradually increased if necessary. The usual daily dose ranges from 200 mg to 2400 mg, divided into two or three doses per day.

For intravenous administration, the dosage is carefully controlled and monitored in a clinical setting. It’s crucial to follow the prescriber’s instructions precisely and never adjust the dose without medical supervision.

Precautions and Warnings for Labetalol Use

While Labetalol is an effective medication for managing hypertension, certain precautions should be taken to ensure safe use.

Who should avoid taking Labetalol?

Labetalol may not be suitable for everyone. It should be avoided or used with caution in patients with:

• Severe bradycardia (slow heart rate)
• Heart block greater than first degree
• Cardiogenic shock
• Severe liver disease
• Known hypersensitivity to Labetalol or any of its components

Pregnant women and nursing mothers should consult their healthcare provider before using Labetalol, as it may pose risks to the fetus or infant.

What precautions should be taken when using Labetalol?

Patients taking Labetalol should be aware of the following precautions:

1. Monitor blood pressure regularly, especially when starting treatment or adjusting the dose.
2. Avoid sudden discontinuation of the medication, as this can lead to rebound hypertension.
3. Be cautious when driving or operating machinery, as Labetalol can cause dizziness.
4. Inform all healthcare providers about Labetalol use before any medical procedures or surgeries.
5. Be aware of potential drug interactions with other medications.

Potential Drug Interactions with Labetalol

Labetalol can interact with various medications, potentially altering its effectiveness or increasing the risk of side effects.

Which medications may interact with Labetalol?

Some medications that may interact with Labetalol include:

• Other blood pressure medications
• Calcium channel blockers
• Antidepressants
• Antidiabetic medications
• Nonsteroidal anti-inflammatory drugs (NSAIDs)
• Certain anesthetics

It’s crucial to inform your healthcare provider about all medications, including over-the-counter drugs and supplements, that you’re taking to avoid potential interactions.

Monitoring and Managing Side Effects of Labetalol

While many side effects of Labetalol are mild and transient, it’s important to monitor for any adverse reactions and manage them appropriately.

How can the side effects of Labetalol be managed?

Here are some strategies for managing common side effects:

• Dizziness: Rise slowly from a sitting or lying position, especially when first starting the medication.
• Fatigue: Ensure adequate rest and discuss with your doctor if fatigue persists or worsens.
• Nausea: Take the medication with food if nausea occurs.
• Nasal stuffiness: Use a saline nasal spray or consult your doctor for appropriate treatment.

If side effects persist or worsen, consult your healthcare provider. They may adjust your dosage or recommend alternative treatments.

Long-term Use and Effectiveness of Labetalol

Labetalol is often prescribed for long-term use in managing hypertension. Understanding its long-term effects and effectiveness is crucial for patients on this medication.

How effective is Labetalol in long-term blood pressure management?

Labetalol has shown to be effective in long-term blood pressure management for many patients. Its dual action on both alpha and beta receptors provides comprehensive blood pressure control. However, the effectiveness can vary among individuals, and regular monitoring is essential to ensure optimal results.

Long-term studies have demonstrated that Labetalol can maintain its blood pressure-lowering effects over extended periods, with many patients achieving and maintaining their target blood pressure levels. The medication’s ability to reduce both systolic and diastolic blood pressure makes it particularly useful in managing various forms of hypertension.

Are there any concerns with long-term use of Labetalol?

While Labetalol is generally well-tolerated for long-term use, there are some considerations:

• Regular monitoring of liver function may be necessary, as Labetalol can rarely cause liver issues.
• Patients with diabetes should monitor their blood sugar levels closely, as Labetalol can mask symptoms of hypoglycemia.
• Long-term use may require periodic reassessment of dosage and effectiveness.
• Some patients may develop tolerance over time, necessitating dosage adjustments.

It’s important to maintain regular check-ups with your healthcare provider to monitor the medication’s effectiveness and any potential long-term effects.

Special Considerations for Labetalol Use in Specific Populations

Certain populations may require special considerations when using Labetalol. Understanding these can help ensure safe and effective use of the medication.

How is Labetalol used in pregnancy and breastfeeding?

Labetalol is often considered a preferred antihypertensive medication during pregnancy, particularly for managing preeclampsia. However, its use should be carefully monitored:

• Pregnancy: Labetalol is classified as Category C, meaning it should be used only if the potential benefit justifies the potential risk to the fetus.
• Breastfeeding: Labetalol does pass into breast milk. While it’s generally considered compatible with breastfeeding, infants should be monitored for potential effects.

Always consult with a healthcare provider for personalized advice regarding Labetalol use during pregnancy or breastfeeding.

What considerations are there for elderly patients using Labetalol?

Elderly patients may be more sensitive to the effects of Labetalol and may require special considerations:

• Lower starting doses may be recommended to minimize the risk of side effects.
• Closer monitoring of blood pressure and heart rate may be necessary.
• Potential interactions with other medications commonly used by elderly patients should be carefully evaluated.

Healthcare providers should assess the benefits and risks of Labetalol use in elderly patients on an individual basis.

Emergency Situations and Labetalol Use

Understanding when to seek immediate medical attention while on Labetalol is crucial for patient safety.

When should you seek immediate medical attention while taking Labetalol?

Seek emergency medical care if you experience any of the following while taking Labetalol:

• Severe dizziness or fainting
• Chest pain or irregular heartbeat
• Difficulty breathing or wheezing
• Swelling of the face, lips, tongue, or throat
• Signs of liver problems (yellowing of skin or eyes, dark urine, persistent nausea)
• Severe skin reactions

These symptoms could indicate serious adverse reactions and require immediate medical evaluation.

How is Labetalol used in hypertensive emergencies?

In hypertensive emergencies, intravenous Labetalol may be used in a controlled clinical setting:

• It can rapidly reduce blood pressure in emergency situations.
• The dosage is carefully titrated based on the patient’s response.
• Close monitoring of blood pressure and heart rate is essential during administration.

Only healthcare professionals should administer intravenous Labetalol in emergency situations.

In conclusion, Labetalol HCl is a powerful and effective medication for managing hypertension. While it offers significant benefits, it’s crucial to be aware of potential side effects, necessary precautions, and situations requiring medical attention. Regular communication with healthcare providers and adherence to prescribed regimens can help ensure safe and effective use of this medication. As with any medical treatment, individualized care and monitoring are key to achieving optimal outcomes with Labetalol therapy.

Side Effects of Trandate (Labetalol), Warnings, Uses

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Labetalol Hydrochloride Side Effects, Adverse Reactions | Healthgrades

Labetalol hydrochloride injection is usually well tolerated. Most adverse effects have been mild and transient and, in controlled trials involving 92 patients, did not require labetalol HCl withdrawal. Symptomatic postural hypotension (incidence, 58%) is likely to occur if patients are tilted or allowed to assume the upright position within 3 hours of receiving labetalol hydrochloride injection. Moderate hypotension occurred in 1 of 100 patients while supine. Increased sweating was noted in 4 of 100 patients, and flushing occurred in 1 of 100 patients.

The following also were reported with labetalol hydrochloride injection with the incidence per 100 patients as noted:

Cardiovascular System: Ventricular arrhythmia in 1.

Central and Peripheral Nervous Systems: Dizziness in 9, tingling of the scalp/skin in 7, hypoesthesia (numbness) and vertigo in 1 each.

Gastrointestinal System: Nausea in 13, vomiting in 4, dyspepsia and taste distortion in 1 each.

Metabolic Disorders: Transient increases in blood urea nitrogen and serum creatinine levels occurred in 8 of 100 patients; these were associated with drops in blood pressure, generally in patients with prior renal insufficiency.

Psychiatric Disorders: Somnolence/yawning in 3.

Respiratory System: Wheezing in 1.

Skin: Pruritus in 1.

The incidence of adverse reactions depends upon the dose of labetalol HCl. The largest experience is with oral labetalol HCl (see Labetalol Hydrochloride Tablets Product Information for details). Certain of the side effects increased with increasing oral dose, as shown in the following table that depicts the entire US therapeutic trials data base for adverse reactions that are clearly or possibly dose related.

In addition, a number of other less common adverse events have been reported: 

Cardiovascular: Hypotension, and rarely, syncope, bradycardia, heart block.

Liver and Biliary System: Hepatic necrosis, hepatitis, cholestatic jaundice, elevated liver function tests.

Hypersensitivity: Rare reports of hypersensitivity (e.g., rash, urticaria, pruritus, angioedema, dyspnea) and anaphylactoid reactions.

The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with labetalol HCl during investigational use and extensive foreign marketing experience.

clinical laboratory tests

Among patients dosed with labetalol hydrochloride tablets, there have been reversible increases of serum transaminases in 4% of patients tested and, more rarely, reversible increases in blood urea.

Labetalol: a review of its pharmacology, pharmacokinetics, clinical uses and adverse effects

Labetalol is a combined alpha- and beta-adrenoceptor blocking agent for oral and intravenous use in the treatment of hypertension. It is a nonselective antagonist at beta-adrenoceptors and a competitive antagonist of postsynaptic alpha 1-adrenoceptors. Labetalol is more potent at beta that at alpha 1 adrenoceptors in man; the ratio of beta-alpha antagonism is 3:1 after oral and 6.9:1 after intravenous administration. Labetalol is readily absorbed in man after oral administration, but the drug, which is lipid soluble, undergoes considerable hepatic first-pass metabolism and has an absolute bioavailability of approximately 25%. There are no active metabolites, and the elimination half-life of the drug is approximately 6 hours. Unlike conventional beta-adrenoceptor blocking drugs without intrinsic sympathomimetic activity, labetalol, when given acutely, produces a decrease in peripheral vascular resistance and blood pressure with little alteration in heart rate or cardiac output. However, like conventional beta-blockers, labetalol may influence the renin-angiotensin-aldosterone system and respiratory function. Clinical studies have shown that the antihypertensive efficacy of labetalol is superior to placebo and to diuretic therapy and is at least comparable to that of conventional beta-blockers, methyldopa, clonidine and various adrenergic neuronal blockers. Labetalol administered alone or with a diuretic is often effective when other antihypertensive regimens have failed. Studies have shown that labetalol is effective in the treatment of essential hypertension, renal hypertension, pheochromocytoma, pregnancy hypertension and hypertensive emergencies. In addition, preliminary studies indicate that labetalol may be of value in the management of ischemic heart disease. The most troublesome side effect of labetalol therapy is posture-related dizziness. Other reported side effects of the drug include gastrointestinal disturbances, tiredness, headache, scalp tingling, skin rashes, urinary retention and impotence. Side effects related to the beta-adrenoceptor blocking effect of labetalol, including asthma, heart failure and Raynaud’s phenomenon, have been reported in rare instances.

Labetalol 200 mg Film-coated Tablets – Summary of Product Characteristics (SmPC)

This information is intended for use by health professionals

Labetalol 200 mg Film-coated Tablets

Each film-coated tablet contains 200 mg labetalol hydrochloride

Excipients with known effect

Each film-coated tablet contains 15. 0 mg sucrose.

For the full list of excipients, see section 6.1

Round orange biconvex film-coated tablets marked “LL 200” on one side and blank on the other.

Labetalol is a combined alpha and beta-adrenoceptor blocker indicated for:

– Hypertension, including hypertension in pregnancy.

– Angina pectoris with existing hypertension.

For oral administration only.

Labetalol tablets should be taken with food.

Adults:

Hypertension: Initially, 100 mg twice daily. In patients already being treated with antihypertensives and in those of low body weight this may be sufficient to control blood pressure. In others, increases in dose of 100 mg twice daily should be made at intervals of 14 days. Many patients blood pressure is controlled by 200 mg twice daily. If necessary up to 800 mg daily may be given, as a twice daily regimen. In severe refractory hypertension, daily doses of up to 2400 mg have been given, divided into three or four times a day regimens.

Hypertension in Pregnancy: An initial dosage of 100 mg twice daily may be increased, if necessary at weekly intervals by 100 mg twice daily. During the second and third trimesters, the severity of hypertension may necessitate a further dose titration to a three times daily regimen ranging from 100 mg – 400 mg three times a day. The total daily dosage should not exceed 2400 mg.

Hospital in-patients with severe hypertension, particularly in pregnancy, may have daily increases in dosage.

Angina Co-Existing with Hypertension: The recommended dose is that which is necessary to control the hypertension.

Paediatric population:

Labetalol is not recommended for use in children due to a lack of data on safety and efficacy.

Elderly:

An initial dose of 50 mg twice daily is recommended and this has been sufficient in some cases to control hypertension.

General

Additive hypotensive effects may be expected if Labetalol tablets are administered together with other antihypertensives e. g. diuretics, methyldopa etc. When transferring patients from such agents, Labetalol tablets should be introduced with a dosage of 100 mg twice daily and the previous therapy gradually decreased. Abrupt withdrawal of clonidine or beta-blocking agents is undesirable.

– Hypersensitivity to labetalol hydrochloride or to any of the tablet excipients listed in section 6.1

– Second or third degree heart block

– Cardiogenic shock

– Uncontrolled, incipient or digitalis-refractory heart failure

– Sick sinus syndrome (including sino-atrial block)

– Hypotension

– Untreated phaeochromocytoma

– Severe peripheral circulatory disturbances

– Bradycardia (<45-50 bpm)

– History of bronchspasm or chronic obstructive airways disease

– After prolonged fasting

– Prinzmetal’s angina

– Metabolic acidosis (e.g. in some diabetics).

There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenoceptor blocking drugs. The reported incidence is small and in most cases the symptoms have cleared when the treatment was withdrawn. Gradual discontinuance of the drug should be considered if any such reaction is not otherwise explicable.

There have been reports of severe hepatocellular injury with Labetalol therapy which has occurred after both short-term and long-term treatment and is usually reversible upon withdrawal of the drug. At the first sign or symptom of liver dysfunction appropriate laboratory testing should be carried out. If there is laboratory evidence of liver injury or the patient is jaundiced, Labetalol should be stopped and not re-started.

Particular care should be taken when labetalol is used in patients with hepatic impairment as these patients metabolise labetalol more slowly than patients without hepatic impairment. Lower doses may be required.

The occurrence of Intraoperative Floppy Iris Syndrome (IFIS, a variation of Small Pupil Syndrome) has been observed during cataract surgery in some patients on, or previously treated with, tamsulosin. Isolated reports have also been received with other alpha-1 blockers and the possibility of a class effect cannot be excluded. As IFIS may lead to increased procedural complications during the cataract operation, current or past use of alpha-1 blockers should be made known to the ophthalmic surgeon in advance of surgery.

Beta-adrenoceptor blocking drugs reduce cardiac output through their negative inotropic and negative chronotropic effects. Beta-blockers may therefore cause worsening systolic heart failure or the development of heart failure in patients who depend on high sympathetic drive to maintain cardiac output.

Especially in patients with ischaemic heart disease, sudden withdrawal of beta-adrenoceptor blocking drugs may result in anginal attacks of increased frequency or severity. Therefore, withdrawal of Labetalol in patients with ischaemic heart disease should be gradual i.e. over 1-2 weeks, and if necessary at the same time initiating replacement therapy, to prevent exacerbation of angina pectoris. In addition, hypertension and arrhythmias may develop.

Particular care is required with patients whose cardiac reserve is poor. Beta-adrenoceptor blocking drugs should be avoided in overt heart failure or poor left ventricular systolic function, although they may be used when cardiac failure has been controlled.

A reduction in heart rate (bradycardia) is a pharmacological effect of Labetalol. In rare cases where symptoms may be attributable to the heart rate decreasing to less than 50-55 beats per minute at rest, the dose should be reduced.

Airway obstructions may be aggravated in patients with chronic obstructive pulmonary disorders. Non-selective beta-blockers, such as Labetalol, should not be used for these patients unless no alternative treatment is available. In such cases the risk of inducing bronchospasm should be appreciated and appropriate precautions taken. If bronchospasm should occur after the use of Labetalol it can be treated with a beta2-agonist by inhalation, e. g. salbutamol (the dose of which may need to be greater than the usual in asthma) and, if necessary, intravenous atropine 1 mg.

Labetalol should only be given with caution to patients with first-degree heart block due to its negative effect on conduction time. Patients with liver or kidney insufficiency may need a lower dosage, depending on the pharmacokinetic profile of the compound. Tolerance to Labetalol is usually good in the elderly, however, they should be treated with caution and with a lower starting dose.

Beta adrenoceptor blocking drugs may increase the number and duration of anginal attacks in patients with Prinzmetal’s angina, due to unopposed alpha-receptor mediated coronary artery vasoconstriction. Non-selective beta-blockers, such as Labetalol, should not be used for these patients.

Patients with a history of psoriasis should only be administered beta adrenoceptor blockers after careful consideration.

There have been reports of increased sensitivity towards allergens and the seriousness of anaphylactic reactions with the use of beta adrenoceptor blocking drugs. While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.

Labetalol modifies the tachycardia of hypoglycaemia and it may prolong the hypoglycaemic response to insulin. Care should be exercised during concomitant use of Labetalol and hypoglycaemic therapy in patients with diabetes mellitus.

As with other beta-adrenoceptor blocking drugs, labetalol may mask the symptoms of hypoglycaemia in diabetic patients and thyrotoxicosis.

Care is required when transferring patients from clonidine to a beta-adrenoceptor blocking drug. Labetalol should be introduced with a dosage of 100 mg twice daily and clonidine gradually decreased. Labetalol may prove useful in preventing rebound hypertension following clonidine withdrawal.

Because of negative inotropic effects, care is required when prescribing a beta-adrenoceptor blocking drug with class 1 antidysrhythmic agents such as disopyramide.

Beta-adrenoceptor blocking drugs should be used with caution in combination with verapamil where ventricular function is impaired. The combination should not be given to patients with conduction abnormalities, nor should either drug be administered intravenously within 48 hours of discontinuing the other.

Care is required during parenteral administration of preparations containing adrenaline to patients receiving beta-adrenoceptor blocking drugs, as in rare instances vasoconstriction, hypertension and bradycardia may occur. A reduced dosage of adrenaline should be used.

Beta-blockade therapy should be discontinued for at least 24 hours if it is decided to interrupt it prior to surgery. Continuation of beta-blockade during surgery reduces the risk of arrhythmias during induction and intubation but may increase the risk of hypertension.

Great care should be taken with patients with peripheral circulatory disorders such as Raynaud’s disease or syndrome or intermittent claudication. Beta adrenoceptor blockers may lead to the aggravation of such disorders.

Care is required when administering anaesthetic agents to patients receiving Labetalol. The anaesthetist should always be informed of the use of a beta-adrenoceptor blocking drug. The risks and benefits of continued beta-adrenoceptor blocking therapy in the peri-operative period should be carefully evaluated. Halothane in high concentrations (≥3%) and other halogenated hydrocarbon anaesthetics should be avoided with Labetalol due to risk of excessive hypotension, large decrease in cardiac output and increase in central venous pressure. Patients should receive intravenous atropine prior to induction. During anaesthesia Labetalol may mask the compensatory physiological responses to sudden haemorrhage (tachycardia and vasoconstriction). Close attention must therefore be paid to blood loss and the blood volume maintained.

The presence of Labetalol metabolites in the urine may result in falsely elevated levels of urinary catecholamines, metaneprine, normataneprine and vanillylmandelic acid when measured by flourometric or photometric methods.

In patients with phaeochromocytoma, labetalol may be administered only after adequate alpha-blockade is achieved.

All labelling for Labetalol will carry the following warning:

Do not take this medicine if you have wheezing or asthma.

This medicine contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.

This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially ‘sodium-free’.

Tricyclic antidepressants, barbiturates and phenothiazines as well as other antihypertensive agents will potentate the hypotensive action of Labetalol. Concomitant use of tricyclic antidepressants may increase the incidence of tremor.

Parenteral administration of preparations containing sympathomimetics, such as adrenaline, to patients taking beta-adrenoceptor blocking drugs, may in rare cases, result in vasoconstriction, hypertension and bradycardia (see section 4. 4). Labetalol is less likely to cause acute hypertensive reactions than other beta-blockers due to its alpha-blocking activity.

Beta-adrenoceptor blocking drugs may enhance the negative inotropic and chronotropic actions of verapamil, and to a lesser extent diltiazem. Therefore, concurrent use is not recommended.

Care should be taken if beta adrenoceptor blocking drugs are used in conjunction with Class 1 anti-arrhythmic agents such as disopyramide, quinidine and amiodarone, as they may have a potentiating effect on atrial-conduction time and induce a negative inotropic effect.

Beta adrenoceptor blockers should not be used in conjunction with digitalis glycosides as they may increase auriculo-ventricular conduction time.

Non selective beta-blockers increase the risk of “rebound hypertension” when used in conjunction with clonidine. Treatment with clonidine should be continued for some time after treatment with the beta-blocker has been discontinued.

Beta adrenoceptor blocking drugs should not be used concomitantly with monamine oxidase inhibitors (MAOIs) with the exception of MAO-B inhibitors.

Administration of anaesthetic drugs with beta adrenoceptor drugs may lead to attenuation of the reflex tachycardia and increase the risk of hypotension. Continuation of beta-blockers reduces the risk of arrhythmia during induction and intubation. The anaesthetist should be informed when the patient is receiving a beta-blocking agent. Anaesthetic agents which can cause myocardial depression, such as cyclopropane and trichlorethylene, should be avoided.

Beta-blockers may enhance hypoglycaemic effects of antidiabetic agents and mask the warning signs of hypoglycaemia such as tremor and tachycardia.

Cimetidine, hydralazine and alcohol increase the bioavailability of beta-blockers which are mainly metabolised by the liver; The effect of Labetalol may therefore be potentiated by concomitant treatment with these drugs.

Beta-blockers, when used with dihydropyridine derivatives such as nifedipine, increase the risk of hypotension. In patients with latent cardiac insufficiency, treatment with beta-blocking agents may lead to cardiac failure.

Prostaglandin synthetase inhibiting drugs may decrease the hypotensive effects of beta-blockers. Dosage adjustments may therefore be necessary.

The central depressant effect of alcohol, analgesics and tricyclic antidepressants is potentiated.

Several different drugs or drug classes may enhance the hypotensive effects of labetalol: ACE inhibitors; angiotensin-II antagonists; aldesleukin, alprostadil; anxiolytics; hypnotics; moxisylyte; diuretics; alpha-blockers.

Several different drugs or drug classes may antagonise the hypotensive effects of labetalol: NSAIDs, corticosteroids; oestrogens; progesterones.

Labetalol has been shown to reduce the uptake of radioisotopes of metaiodobenzylguanidine (MIBG), and may increase the likelihood of a false negative study. Care should therefore be taken in interpreting results from MIBG scintigraphy. Consideration should be given to withdrawing labetalol for several days at least before MIBG scintigraphy, and substituting other beta or alpha-blocking drugs.

Antimalarials such as mefloquine or quinine may increase the risk of bradycardia.

Ergot derivatives may increase the risk of peripheral vasoconstriction.

Pregnancy

While no teratogenic effects have been demonstrated in animals, Labetalol should only be used during the first trimester of pregnancy if the potential benefits are likely to outweigh the possible risk to the foetus.

Labetalol crosses the placental barrier and the possible consequences of alpha- and beta-adrenoceptor blockade in the foetus and neonate should be borne in mind. Perinatal and neonatal distress (bradycardia, hypotension, respiratory depression, hypoglycaemia, hypothermia) has been rarely reported. Sometimes these symptoms have developed a day or two after birth. Response to supportive measures (e.g. intravenous fluids and glucose) is usually prompt but with severe pre-eclampsia, particularly after prolonged intravenous labetalol, recovery may be slower. This may be related to diminished liver metabolism in premature babies.

Beta-blockers reduce placental perfusion, which may result in intrauterine foetal death, immature and premature deliveries.

There is an increased risk of cardiac and pulmonary complications in the neonate in the postnatal period. Intra-uterine and neonatal deaths have been reported with Trandate but other drugs (e.g. vasodilators, respiratory depressants) and the effects of pre- eclampsia, intra-uterine growth retardation and prematurity were implicated. Such clinical experience warns against unduly prolonging high dose labetalol and delaying delivery and against co-administration of hydralazine.

Breast-feeding

Labetalol is excreted in breast milk in small amounts (approximately 0.004% of the maternal dose). Adverse events of unknown causality (sudden death syndrome, diarrhoea, hypoglycaemia) have been reported very rarely in breast-fed neonates. Caution should be exercised when labetalol is administered to breast-feeding women.

No studies on the effects on the ability to drive and use machines have been performed. The use of labetalol is unlikely to result in any impairment. However, when driving or operating machines, it should be taken into account that occasionally dizziness or fatigue may occur.

Most side effects are transient and occur during the first few weeks of treatment with

Labetalol. They include:

Immune system disorders

Very common: Positive antinuclear antibodies unassociated with disease.

Common: Hypersensitivity (rash, pruritus, angioedema and dyspnoea).

Blood and the lymphatic system disorders

Not known: Hyperkalaemia, particularly in patients who may have impaired renal excretion of potassium, thrombocytopenia.

Psychiatric disorders

Not known: Depressed mood and lethargy, hallucinations, psychoses, confusion, sleep disturbances, nightmares.

Nervous system disorders

Common: Dizziness, tingling sensation in scalp usually transient may occur in a few patients early in treatment.

Very rare: Tremor has been reported in the treatment of hypertension of pregnancy.

Not known: Headache, tiredness.

Eye disorders

Not known: Impaired vision, dry eyes.

Cardiac disorders

Common: Heart failure.

Rare: Bradycardia.

Very rare: Heart block

Not known: Hypotension.

Vascular disorders

Very rare: Exacerbation of the symptoms of Raynaud’s Syndrome.

Not known: Ankle oedema, increase of an existing intermittent claudication, postural hypotension is uncommon except at very high doses, or if the initial dose is too high or doses are increased too rapidly.

Respiratory, thoracic and mediastinal disorders

Uncommon: Bronchospasm (in patients with asthma or a history of asthma).

Not known: Nasal congestion, interstitial lung disease.

Gastrointestinal disorders

Not known: Epigastric pain, nausea, vomiting, diarrhoea.

Hepatobiliary disorders

Common: Raised liver function tests.

Very rare: Jaundice (both hepatocellular and cholestatic), hepatitis and hepatic necrosis. When mild, hepatotoxicity is usually reversible on withdrawal of the drug.

Skin and subcutaneous tissue disorders

Not known: Sweating, reversible lichenoid rash, cold or cyanotic extremities, paraesthesia of the extremities, photosensitivity reactions, exacerbation of psoriasis, reversible alopecia.

Musculoskeletal and connective tissue disorders:

Very rare: toxic myopathy, systemic lupus erythematous.

Not known: Cramps. toxic myopathy, systemic lupus erythematous.

Renal and urinary disorders

Common: Difficulty in micturition.

Not known: Acute retention of urine.

Reproductive system and breast disorders

Common: Ejaculatory failure, erectile dysfunction.

General disorders and administration site conditions

Common: Drug fever.

Not known: Masking of the symptoms of thyrotoxicosis or hypoglycaemia.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continual monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reaction via the Yellow Card Scheme, at www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.

Clinical features of overdosage may include bradycardia, hypotension, bronchospasm, acute cardiac insufficiency, hypoglycaemia, delirium and unconsciousness. In the case of large overdosages, beta-blockers can cause a membrane-stabilising action.

After ingestion of an overdose or in case of hypersensitivity, the patient should be kept under close supervision and be treated in an intensive-care ward. Following recent overdose, the stomach should be emptied by gastric aspiration and lavage, administration of activated charcoal and a laxative. Artificial respiration may be required. Bradycardia or extensive vagal reactions should be treated by administering atropine or methylatropine. Hypotension and shock should be treated with plasma/plasma substitutes and, if necessary, catecholamines. The beta-blocking effect can be counteracted by slow intravenous administration of isoprenaline hydrochloride, starting with a dose of approximately 5μg/min, or dobutamine, starting with a dose of 2.5 μg/min, until the required effect has been obtained. In refractory cases isoprenaline can be combined with dopamine. If this does not produce the desired effect either, intravenous administration of 8-10 mg glucagon may be considered. If required the injection should be repeated within one hour, to be followed, if required, by an i.v. infusion of glucagon at an administration rate of 1-3 mg/hour. Administration of calcium ions, or the use of a cardiac pacemaker may also be considered.

Oliguric renal failure has been reported after massive overdosage of labetalol orally. In one case, the use of dopamine to increase the blood pressure may have aggravated the renal failure. Labetalol does have membrane stabilising activity which may have clinical significance in overdosage.

Haemodialysis removes less than 1% labetalol hydrochloride from the circulation.

Pharmatherapeutic group: Alpha and beta blocking agents, ATC code: C07AG01

Labetalol combines selective alpha₁-blocking activity with non-selective beta-blockade. Through alpha-blockade, it reduces peripheral resistance, decreasing myocardial after-load and oxygen demand. Concurrent beta-blockade protects against reflex sympathetic cardiac effects. Cardiac output is not significantly reduced at rest or with moderate exercise. Systolic blood pressure elevation during exercise is reduced, but corresponding changes in diastolic pressure are essentially normal.

In patients with angina pectoris co-existing with hypertension, the reduced peripheral resistance decreases myocardial afterload and oxygen demand. All these effects would be expected to benefit hypertensive patients and those with co-existing angina.

Labetalol is completely absorbed after oral administration. Bioavailabilty is significantly reduced to first-pass metabolism in the liver, but can be enhanced by concurrent administration of food. Peak effects are seen 2-4 hours after dosing and the plasma half-life is 6-8 hours. Labetalol exhibits moderately high (~50%) plasma protein binding. It undergoes hepatic biotransformation with inactive metabolites being excreted in the urine (55-60%) and faeces. Less than 5% of an oral dose is excreted unchanged in the urine.

There is no preclinical safety data of relevance to the prescriber which are additional to those already included in other section of the SPC.

The tablet core contains:

Cellulose, microcrystalline

Starch, pregelatinised

Sucrose

Sodium starch glycolate (Type A)

Silica, colloidal anhydrous

Silica, colloidal hydratedMagnesium stearate.

The film coating (Opadry Orange OY-23003) contains:

Hypromellose

Macrogol 400

Titanium dioxide (E171)

Erythrosine (E127)

Quinoline yellow (E104)

Carnauba Wax

Store in a dry place below 25°C. Store in the original package in order to protect from light.

Polypropylene containers with polyethylene caps (with optional use of polyethylene ullage filler) and PVdC foil blister packs in pack sizes of 5, 7, 10, 14, 15, 20, 21, 25, 28, 30, 56, 60, 84, 90, 100, 112, 120, 168, 180, 250 & 500.

Not all pack sizes may be marketed.

Generics [UK] Limited t/a Mylan

Station Close

Potters Bar

Hertfordshire

EN6 1TL

Date Granted: 19/04/1985

Last Renewal: 19/01/2005

Get Labetalol Prescription Online. Request Labetalol Online Prescription And Get Labetalol HCl 100 mg or 200 mg Tablets Near You.

• Request labetalol online prescription
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Labetalol – Overview

Labetalol is a medication sometimes prescribed to people to help them manage their hypertension. People who might need a labetalol HCl medication prescription, including labetalol 200 mg and labetalol 100 mg tablets, can use Push Health to connect with a local medical provider who can prescribe labetalol when appropriate to do so.

What Is Labetalol Used For?

Labetalol, previously marketed under the brand name Trandate, is a medication sometimes prescribed to people who have hypertension. Labetalol is a type of drug that belongs to a class of medication known as alpha1-adrenergic and beta-adrenergic blockers. Because of this dual activity, labetalol is thought to work by reducing resistance in the blood vessels, partially through relaxing smooth muscle in the vasculature, and reducing heart rate. This dual activity is what makes labetalol different from beta blockers such as atenolol (Tenormin), bisoprolol (Zebeta), metoprolol (Lopressor, Toprol) and nebivolol (Bystolic). Labetalol works better when used in conjunction with other lifestyle measures such as an improved diet and exercise.

Labetalol – Dosage and Cost

Labetalol is typically started at labetalol 100 mg twice per day although the starting regimen depends on the health characteristics of the patient and the judgement of the prescribing medical provider. The dose of labetalol used may be titrated from there based on the response of the patient to the medication. Following oral administration, labetalol generally exhibits a half life of under 8 hours when given to healthy individuals. Labetalol is excreted in both the urine and the feces. Generic labetalol is affordable, costing approximately 30 cents or less at most pharmacies in the United States. Labetalol coupons are sometimes available from various sources and some insurance plans will cover the costs associated with labetalol, depending on why it was prescribed and the insurance coverage.

Can I Buy Labetalol Online?

Labetalol OTC is not available and one cannot just buy labetalol online as labetalol requires a prescription to be dispensed by a pharmacy in the United States. Because of this, the first step to getting a labetalol medication prescription is consulting a licensed medical provider. People who might need a labetalol prescription can use Push Health to connect with a local medical provider who, when appropriate, can prescribe labetalol HCl tablets.

Labetalol – Side Effects

Labetalol medication can cause adverse effects when used and labetalol’s side effects should be discussed with a qualified medical practitioner while using the medication. Side effects that can result from labetalol HCl use include low blood pressure, fatigue, headache, nausea, vomiting, heartburn, dizziness and drowsiness. People with liver problems or certain types of heart conditions should not use labetalol. Labetalol prescription tablets can interact with other drugs and care should be taken when prescribed as part of a wider medication regimen. Labetalol and alcohol should not be used together. People with a known hypersensitivity to labetalol prescription medication or similar drugs should not use labetalol tablets.

More Labetalol Information

Last updated June 2, 2021. Given the evolving nature of medicine and science, this information might not be accurate and should not be construed as medical advice or diagnosis / treatment recommendations. Please consult a licensed medical provider if you have additional questions.

Canadian Pharmacy: Buy Trandate Online

Trandate Product Description

Drug Uses

Trandate is an antihypertensive medication used for the management of all grades of hypertension. Trandate can be used for initial monotherapy of hypertension or as an “add-on” antihypertensive therapy. Trandate is different from other types of antihypertensive medications by that it rarely causes postural hypotension and provides a significant antihypertensive effect:

• without reflex tachycardia

• without cardiac stimulation
• without reduction in heart rate

The maximum maintenance dose of Trandate for the treatment of mild to moderate essential hypertension is 400mg in two divided doses. To treat severe essential hypertension, an increase in the total daily dose of Trandate up to 2.4g in divided doses can be required.

Missed Dose

If you forget to use your usual dose of Trandate, take it as soon as possible only if there is much time until the next planned dose of this antihypertensive agent. Trandate doses must be spaced, do not use two tablets of the same antihypertensive agent together.

More Information

For the treatment of severe hypertension at home, Trandate is advised to use in combination with diuretics (including thiazides, loop diuretics) and / or other medications to lower high blood pressure. For the treatment of acute hypertensive episodes in hospitalized patients, Trandate intravenous injections or infusions should be used.

Storage

Trandate must be stored at room temperature not above 30°C. It is recommended to keep Trandate tablets in the original package in order to protect from light and moisture.

Trandate Safety Information

Warnings

Trandate may cause slowly progressive, reversible hepatic injury in some patients. Because of potential risk of severe hepatocellular injury, hypertensive patients using Trandate require periodic assessment of liver function.

Disclaimer

All available information about hypertension presented in Trandate review should not be considered as a substitute for consultation with or treatment offered by primary health care practitioner. The online pharmacy assumes no responsibility for any claim connected with how and for what purpose information about Trandate antihypertensive agent was used.

Trandate Side Effects

Mainly, Trandate is well tolerated. The intensity of Trandate adverse effects depends on the dosage of this antihypertensive agent. The most common adverse effects of Trandate include vomiting, dyspepsia, nasal stuffiness, impotence, fatigue, paresthesia, ejaculation failure, nausea, edema and dizziness. Less than 10% of cases of refusal to use Trandate because of serious adverse effects are registered.

Canadian Pharmacy: Buy Trandate Online

Trandate Product Description

Drug Uses

Trandate is an antihypertensive medication used for the management of all grades of hypertension. Trandate can be used for initial monotherapy of hypertension or as an “add-on” antihypertensive therapy. Trandate is different from other types of antihypertensive medications by that it rarely causes postural hypotension and provides a significant antihypertensive effect:

• without reflex tachycardia

• without cardiac stimulation
• without reduction in heart rate

The maximum maintenance dose of Trandate for the treatment of mild to moderate essential hypertension is 400mg in two divided doses. To treat severe essential hypertension, an increase in the total daily dose of Trandate up to 2.4g in divided doses can be required.

Missed Dose

If you forget to use your usual dose of Trandate, take it as soon as possible only if there is much time until the next planned dose of this antihypertensive agent. Trandate doses must be spaced, do not use two tablets of the same antihypertensive agent together.

More Information

For the treatment of severe hypertension at home, Trandate is advised to use in combination with diuretics (including thiazides, loop diuretics) and / or other medications to lower high blood pressure. For the treatment of acute hypertensive episodes in hospitalized patients, Trandate intravenous injections or infusions should be used.

Storage

Trandate must be stored at room temperature not above 30°C. It is recommended to keep Trandate tablets in the original package in order to protect from light and moisture.

Trandate Safety Information

Warnings

Trandate may cause slowly progressive, reversible hepatic injury in some patients. Because of potential risk of severe hepatocellular injury, hypertensive patients using Trandate require periodic assessment of liver function.

Disclaimer

All available information about hypertension presented in Trandate review should not be considered as a substitute for consultation with or treatment offered by primary health care practitioner. The online pharmacy assumes no responsibility for any claim connected with how and for what purpose information about Trandate antihypertensive agent was used.

Trandate Side Effects

Mainly, Trandate is well tolerated. The intensity of Trandate adverse effects depends on the dosage of this antihypertensive agent. The most common adverse effects of Trandate include vomiting, dyspepsia, nasal stuffiness, impotence, fatigue, paresthesia, ejaculation failure, nausea, edema and dizziness. Less than 10% of cases of refusal to use Trandate because of serious adverse effects are registered.

90,000 Publications in the media

(Labetalolum) INN

Synonyms. Trandat.

Composition and form of release. Tablets of 0.1 and 0.2 g labetalol; 1% solution of labetalol for injection in ampoules of 5 ml.

Indications. Hypertension of varying degrees.

Pharmacological action. An antiadrenergic agent that blocks beta and alpha 1-adrenergic receptors, leading to vasodilation, a decrease in systemic vascular resistance and practically not causing postural hypotension. The drug does not significantly affect cardiac output and heart rate. The maximum effect from the use of the drug is observed after 1 hour to 4 hours after administration and lasts up to 8-12 hours or up to 24 hours when using high doses.

Pharmacokinetics. Labetalol is almost completely absorbed from the gastrointestinal tract into the blood, but undergoes active “first-pass metabolism”, and its bioavailability is 25%. The maximum concentration in the blood is reached within 2-4 hours after a single oral dose.The drug binds to blood proteins by 50%. T 1/2 is 6-8 hours. Labetalol is metabolized in the liver and excreted from the body through the gastrointestinal tract, 55-60% – in the urine.

Side effects. Heart failure, bronchospasm, hypoglycemia, dizziness, headache, nausea, vomiting, diarrhea or constipation, feeling tired.

Contraindications. Severe heart failure, AV block.

Adverse reactions when interacting with other drugs. Hypotension may develop when used together with other antihypertensive drugs or diuretics. With the combined use of labetalol with halogen-containing general anesthetics, excessive hypotension may develop, a significant decrease in cardiac output and an increase in central venous pressure. Cimetidine increases the plasma concentration of labetalol when used together. Estrogens reduce the hypotensive effect of labetalol. Labetalol reduces reflex tachycardia caused by nitroglycerin and increases the hypotensive effect.When using phenothiazines with labetalol, the plasma concentration of these drugs increases. Propafenone increases the plasma concentration and T 1/2 of labetalol.

Information for the patient. Labetalol is taken at 0.1 g 2-3 times a day after meals, mixed with liquid (water, juices), non-solid food (applesauce, pudding). The dose can be increased if necessary. In hypertensive crises, the drug is used intravenously. Care should be taken when using the drug for bronchial asthma. The drug is withdrawn gradually. Take the missed dose as soon as possible and do not take it at all if there are less than 4 hours left until the next dose; do not take double doses.

Labetalol :: Instruction :: Price :: Description of the drug

Labetalol (Labetalol)
Refers to “hybrid” adrenergic blockers that block both beta and alpha adrenergic receptors.
The combination of beta-adrenoceptor blocking and peripheral vasodilator (vasodilator) action provides a reliable antihypertensive (blood pressure lowering) effect.The drug does not significantly affect the value of cardiac output and heart rate.
Labetalol is used to lower blood pressure in hypertension (rise in blood pressure) of varying degrees. Unlike conventional beta-blockers, it has a rapid antihypertensive effect.
Inside appoint in the form of tablets (with meals), 0.1 g (100 mg) 2-3 times a day. In severe forms of hypertension, the dose is increased. The average daily dose is 600-1000 mg in 2-4 doses. For maintenance therapy, 1 tablet (100 mg) is used 2 times a day.
In hypertensive crises (rapid and sharp rise in blood pressure), labetalol is slowly administered intravenously at a dose of 20 mg (2 ml of a 1% solution). If necessary, repeat injections at intervals of 10 minutes. It is preferred to administer labetalol by infusion. To do this, dilute 1% injection solution in ampoules with isotonic sodium chloride or glucose solution to a concentration of 1 mg / ml. Injected at a rate of 2 ml (2 mg) per minute. Usually the required dose is 50-200 mg.
Intravenous administration is performed in a hospital (hospital) with the patient lying down (due to a rapid and significant decrease in blood pressure).
When using labetalol, dizziness, headache, nausea, constipation or diarrhea, fatigue, itching are possible.
Labetalol is contraindicated in patients with severe heart failure, atrioventricular block (impaired conduction of excitation through the heart).
Bronchospasm (a sharp narrowing of the lumen of the bronchi) the drug usually does not cause, however, in patients with bronchial asthma, caution should be exercised.
Tablets of 0.1 and 0.2 g (100 and 200 mg), 30 and 100 pieces per package; 1% solution for injection in ampoules of 5 ml (50 mg in an ampoule).
List B. In the dark place.
Abetol, Albetol, Amipress, Ipolab, Labetol, Labrocol, Lamitol. Operkol, Presolol, Trandat, Trandol.

The manual was compiled by a team of authors and editors of the Piluli website. The list of authors of the reference book of medicines is presented on the page of the site editorial office: Site editorial board.

References to used sources of information.

Description of the drug “ Labetalol ” on this page is a simplified and supplemented version of the official instructions for use.Before purchasing or using the drug, you should consult your doctor and familiarize yourself with the annotation approved by the manufacturer.
Information on the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide on the appointment of the drug, as well as determine the doses and methods of its use.

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LABETALOL (Labetalol) – Information – medical portal of Chelyabinsk

!

Synonyms: Abetol, Albetol, Amipress, Ipolab, Labetol, Labrocol, Lamitol, Opercol, Presolol, Trandat, Trandol, etc.

Pharmacological action. Labetalol is a beta-blocker that simultaneously has an alpha-adrenergic blocking effect.

The combination of beta-adrenergic blocking and peripheral vasodilator (vasodilator) action provides a reliable antihypertensive (blood pressure lowering) effect. The drug does not significantly affect the value of cardiac output and heart rate.

Indication for use. Labetalol is used to lower blood pressure in hypertension

(rise in blood pressure) of varying degrees. Unlike conventional beta-blockers, it has a rapid antihypertensive effect.

Method of administration and dosage. Inside appoint in the form of tablets (with meals), 0.1 g (100 mg) 2-3 times a day. In severe forms of hypertension, the dose is increased. The average daily dose is 600-1000 mg in 2-4 doses. For maintenance therapy, 1 tablet (100 mg) is used 2 times a day.

In hypertensive crises (rapid and sharp rise in blood pressure), labetalol is slowly administered intravenously at a dose of 20 mg (2 ml of a 1% solution). If necessary, repeat injections at intervals of 10 minutes. It is preferred to administer labetalol by infusion. To do this, dilute 1% injection solution in ampoules with isotonic sodium chloride or glucose solution to a concentration of 1 mg / ml. Injected at a rate of 2 ml (2 mg) per minute. Usually the required dose is 50-200 mg.

Intravenous administrations are performed in a hospital (hospital) with the patient lying down (due to a rapid and significant decrease in blood pressure).

Side effects. When using labetalol, dizziness, headache, nausea, constipation or diarrhea, fatigue, itching are possible.

Contraindications. Labetalol is contraindicated in patients with severe heart failure, atrioventricular block (impaired conduction of excitation through the heart).

Bronchospasm (narrowing of the lumen of the bronchi) the drug usually does not cause, however, in patients with bronchial asthma, caution should be exercised.

Form of issue. Tablets of 0.1 and 0.2 g (100 and 200 mg), 30 and 100 pieces per package; 1% solution for injection in ampoules of 5 ml (50 mg in an ampoule).

Storage conditions. List B. In the dark place.

Print version

This information is not a guide to self-treatment. Medical advice required.

PHARMACOLOGICAL EXAM TESTS – Tests

Labetalol – Cardiologist – site about heart and vascular diseases

Pharmacological action

Labetalol is a non-selective beta-adrenergic receptor blocker with a selective blocking effect on postsynaptic alpha-1-adrenergic receptors. Due to the presence of two optical centers in the molecule, there are four diastereoisomers of labetalol, which differ in the degree of pharmacological activity. The ratio of beta and alpha-adrenergic blocking activity of racemic labetalol ranges from 3: 1 when taken orally, to 7: 1 when administered intravenously.

As a result of interaction with alpha- and beta-adrenergic receptors, labetalol causes vasodilation and a decrease in systemic vascular resistance, leading to a decrease in systemic blood pressure without a significant decrease in cardiac output and the development of reflex tachycardia.The adverse effect of labetalol on the lipid spectrum of blood plasma is minimal. With systematic use, labetalol reduces the severity of left ventricular myocardial hypertrophy in patients with hypertension. Labetalol has a quinidine-like membrane stabilizing effect, which, however, appears only when labetalol is administered in very high doses. Compared to other beta-adrenergic blockers (eg propranolol), labetalol does not decrease glomerular filtration and renal blood flow.

Pharmacokinetics

After oral administration, labetalol is rapidly and almost completely absorbed.Simultaneous intake with food slows down the absorption of labetalol in the intestine, but increases the absolute bioavailability. It undergoes significant first-pass metabolism in the mucous membrane of the digestive tract and during the initial passage through the liver, due to which only about 25% of the accepted dose of labetalol enters the systemic circulation unchanged. The antihypertensive effect develops within 20 minutes – 2 hours after oral administration, the maximum effect – after 1-4 hours. The duration of the antihypertensive effect is dose-dependent and is 8-24 hours.

The hypotensive effect after intravenous administration develops in 2–5 minutes and reaches its maximum severity in 5–15 minutes; its duration is 2-4 hours. The half-life in patients with normal renal function ranges from 2.5-8 hours. With severe renal failure, labetalol may accumulate.

It is widely distributed in all tissues of the body, crosses the placenta, and is excreted in breast milk. In small quantities, it penetrates the BBB. Extensively metabolized in the liver by glucuronidation.About 30% is excreted in the bile and excreted in the feces, the rest is excreted in the urine (55-60% in the form of metabolites and 5% unchanged).

Indications

Arterial hypertension, hypertensive crisis, pheochromocytoma, dissecting aortic aneurysm, arterial hypotension when clonidine is withdrawn.

Dosing regimen

Inside, the initial dose is 100 mg 2 times a day, the maximum dose is 2,400 mg per day.
In case of hypertensive crisis, it is administered intravenously slowly (within 2 minutes) at a dose of 20 mg (2 ml of 1% pp).If necessary, the introduction is repeated at intervals of 10 minutes. It is preferable to administer labetalol in the form of an infusion on an isotonic solution of sodium chloride or glucose (the concentration of the solution for infusion is 1 mg / ml) at a rate of 2 mg / min. The usual effective dose is 50-200 mg. The total dose for adults with intravenous administration should not exceed 300 mg.

Limited information on use in children. It is recommended to prescribe orally at the rate of 4 mg / kg per day in 2 divided doses with constant monitoring of blood pressure.When administered intravenously, the bolus dose (administered slowly) is 0.2–1 mg / kg. The initial infusion rate is 0.4–1 mg / kg / h, the maximum is no more than 3 mg / kg / h.

Contraindications

Absolute contraindications – AV blockade, severe bradycardia, cardiogenic shock; relative contraindications – BA, COPD, bronchitis, diabetes mellitus, depression, hyperthyroidism, liver disease, severe pseudoparalytic myasthenia gravis, pregnancy, psoriasis, thyrotoxicosis, ventricular dysfunction.

Side effect

Dizziness, hypertension, syncope, orthostatic hypotension (mainly with intravenous injection), sinus bradycardia, AV blockade, increased symptoms of heart failure, headache, fatigue, depression, nightmares, paresthesia, nausea, vomiting, hepatotoxic effect, shortness of breath, sexual dysfunction (impotence, ejaculation disorders, decreased libido, priapism), urinary retention, hypoglycemia, pruritus, xerosis and skin hyperpigmentation, reversible alopecia, exfoliative dermatitis.

Special instructions

Labetalol can mask the symptoms of hypoglycemia (tachycardia, palpitations, tremors).

Prescribe with caution in patients with liver disease; during treatment, it is necessary to periodically monitor the indicators of the functional state of the liver.

May be effective as monotherapy for dissecting aortic aneurysm.

Since T _1/2 labetalol is large enough, continuous infusion is not recommended.

Drug interaction

With the simultaneous use of labetalol with other antihypertensive drugs, an additive effect is observed. When administered with verapamil or diltiazem, the risk of developing AV block increases.

Possible undesirable pharmacodynamic interactions with the combined simultaneous use of labetalol with antidiabetic agents.

Anesthetic agents can potentiate and prolong the hypotensive effect of labetalol.The combination of halothane and labetalol may cause a synergistic hypotensive effect, decrease cardiac output and decrease central venous pressure.