buprenorphine transdermal: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Warnings:

Buprenorphine has a risk for abuse and addiction, which can lead to overdose and death. Buprenorphine may also cause severe, possibly fatal, breathing problems. To lower your risk, your doctor should have you use the smallest dose of buprenorphine that works, and use it for the shortest possible time. See also How to Use section for more information about addiction.

Ask your doctor or pharmacist if you should have naloxone available to treat opioid overdose. Teach your family or household members about the signs of an opioid overdose and how to treat it.

The risk for severe breathing problems is higher when you start this medication and after a dose increase, or if you use the wrong dose/strength or misuse the medication (such as chewing or swallowing the patch). Using this medication with alcohol or other drugs that can cause drowsiness or breathing problems may cause very serious side effects, including death. Be sure you know how to use buprenorphine and what other drugs you should avoid taking with it. See also Drug Interactions section. Get medical help right away if any of these very serious side effects occur: slow/shallow breathing, unusual lightheadedness, severe drowsiness/dizziness, difficulty waking up.

Keep this medicine in a safe place to prevent theft, misuse, or abuse. If someone accidentally swallows or uses this drug, get medical help right away because fatal breathing problems may occur.

Before using this medication, women of childbearing age should talk with their doctor(s) about the risks and benefits. Tell your doctor if you are pregnant or if you plan to become pregnant. During pregnancy, this medication should be used only when clearly needed. It may slightly increase the risk of birth defects if used during the first two months of pregnancy. Also, using it for a long time or in high doses near the expected delivery date may harm the unborn baby. To lessen the risk, use the smallest effective dose for the shortest possible time. Babies born to mothers who use this drug for a long time may develop severe (possibly fatal) withdrawal symptoms. Tell the doctor right away if you notice any symptoms in your newborn baby such as crying that doesn’t stop, slow/shallow breathing, irritability, shaking, vomiting, diarrhea, poor feeding, or difficulty gaining weight.

How to use Buprenorphine Patch, Transdermal Weekly

See also Warning section.

Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using this medication and each time you get a refill. Learn how to properly use, store, and discard the patches. If you have any questions, ask your doctor or pharmacist.

Use this medication on a regular schedule as directed by your doctor, not as needed for sudden (breakthrough) pain. If you are already using an opioid medication, ask your doctor or pharmacist if you should stop or change how you use your other opioid medication. It may take 24 hours or longer before you have pain relief from buprenorphine patches. Other pain relievers (such as acetaminophen, ibuprofen) may also be prescribed. Ask your doctor or pharmacist about using buprenorphine safely with other drugs.

Apply this medication to the skin as directed by your doctor. Do not apply on burns, cuts, irritated skin, or skin that has been exposed to radiation (x-ray treatment). Select a dry, non-hairy area on a flat part of your body, such as the upper chest, sides of the chest, upper back, or upper outer arms. In people unable to think clearly (such as due to dementia), apply the patch on the upper back to lessen the chance it might be removed or placed in the mouth. If there is hair on the skin, use scissors to clip the hair as close as possible to the skin. Do not shave hair since this might cause skin irritation. If needed, use water to clean the area. Do not use soap, oils, lotions, or alcohol on the application site. Dry the skin well before applying the patch.

The patch is usually changed every 7 days. To avoid irritation, apply to a different area each time and do not apply to the same site within 3 weeks. Be sure to remove the old patch before applying a new patch. The used patch should be folded in half with the sticky sides together and properly discarded. If your manufacturer has supplied a patch disposal unit, follow directions for its use.

Do not use the patch if it appears to be broken, cut, or damaged. Remove from the sealed pouch, peel off the protective liner, and apply right away to the skin. Press firmly in place with the palm of the hand for about 15 to 30 seconds, making sure the contact is complete (especially around the edges). If your prescribed dose is for more than one patch, apply them right next to each other but make sure the edges of the patches do not touch or overlap. After applying the patch, wash your hands with water only.

You may bathe, shower, or swim while wearing the patch. If you have problems with the patch not sticking at the application site, you may tape the edges in place with certain kinds of first aid tape. Ask your doctor or pharmacist about which type of tape should be used. If this problem lasts, ask your doctor for advice. If the patch falls off before 7 days, a new patch may be applied to a different skin site. Be sure to let your doctor know if this happens.

If you accidentally touch the sticky layer to your skin or handle a cut or damaged patch, wash the area well with clear water. If the patch comes off and accidentally sticks to the skin of another person, immediately remove the patch, wash the area with water, and get medical help for them right away. Do not use soap, alcohol, or other products to wash the area.

The dosage is based on your medical condition and response to treatment. Do not apply more patches than directed, change them more frequently, or use them for a longer time than prescribed. Your risk for side effects will increase.

Suddenly stopping this medication may cause withdrawal, especially if you have used it for a long time or in high doses. To prevent withdrawal, your doctor may lower your dose slowly. Tell your doctor or pharmacist right away if you have any withdrawal symptoms such as restlessness, mental/mood changes (including anxiety, trouble sleeping, thoughts of suicide), watering eyes, runny nose, nausea, diarrhea, sweating, muscle aches, or sudden changes in behavior.

When this medication is used for a long time, it may not work as well. Talk with your doctor if this medication stops working well.

Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Use this medication exactly as prescribed to lower the risk of addiction. Ask your doctor or pharmacist for more details.

Tell your doctor if your pain does not get better or if it gets worse.

Side Effects

See also Warning section.

Nausea, vomiting, constipation, lightheadedness, dizziness, drowsiness, dry mouth, or headache may occur. Irritation, itching, or redness at the application site may also occur. Some of these side effects may decrease after you have been using this medication for a while. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

To prevent constipation, eat dietary fiber, drink enough water, and exercise. You may also need to take a laxative. Ask your pharmacist which type of laxative is right for you.

To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: interrupted breathing during sleep (sleep apnea), mental/mood changes (such as agitation, confusion, hallucinations), difficulty urinating, swelling/blistering at the patch application site, signs of your adrenal glands not working well (such as unusual tiredness, weight loss).

Get medical help right away if you have any very serious side effects, including: fainting, seizure, slow/shallow breathing, severe drowsiness/difficulty waking up, fast/irregular heartbeat, severe dizziness.

This drug may rarely cause serious liver disease. Get medical help right away if you have any symptoms of liver damage, including: nausea/vomiting that doesn’t stop, dark urine, loss of appetite, yellowing eyes/skin, severe stomach/abdominal pain.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www. fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before using buprenorphine, tell your doctor or pharmacist if you are allergic to it; or to adhesives; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: brain disorders (such as head injury, tumor, seizures), breathing problems (such as asthma, sleep apnea, chronic obstructive pulmonary disease-COPD), kidney disease, liver disease, mental/mood disorders (such as confusion, depression), personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol), stomach/intestinal problems (such as blockage, constipation, diarrhea due to infection, paralytic ileus), difficulty urinating (such as due to enlarged prostate), disease of the pancreas (pancreatitis), gallbladder disease.

Buprenorphine may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using buprenorphine, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using buprenorphine safely.

This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Raising your skin/body temperature may cause overdose. Avoid increasing your skin temperature at or near the application site (for example, using products such as heating pads, electric blankets, hot tubs, heat or tanning lamps). Avoid taking hot baths and sunbathing. Tell your doctor promptly if you develop a fever.

If you are going to have an MRI test, tell testing personnel that you are using this patch. Some patches may contain metals that can cause serious burns during an MRI. Ask your doctor whether you will need to remove your patch before the test and apply a new patch afterward, and how to do so properly.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the effects of this drug, especially confusion, dizziness, drowsiness, slow/shallow breathing, and QT prolongation (see above).

During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Discuss the risks and benefits with your doctor. (See also Warning section.)

This drug passes into breast milk and may have undesirable effects on a nursing infant. Tell the doctor right away if your baby develops unusual sleepiness, difficulty feeding, or trouble breathing. Consult your doctor before breast-feeding.

Consult your pharmacist or physician.

Interactions

See also Warning section.

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug include: certain pain medications (mixed opioid agonist-antagonists such as butorphanol, nalbuphine, pentazocine), naltrexone, samidorphan.

The risk of serious side effects (such as slow/shallow breathing, severe drowsiness/dizziness) may be increased if this medication is used with other products that may also cause drowsiness or breathing problems. Tell your doctor or pharmacist if you are taking other products such as other opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

This medication may interfere with certain laboratory tests (including amylase/lipase levels), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Does Buprenorphine Patch, Transdermal Weekly interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

This medication patch may be harmful if chewed or swallowed. If someone has overdosed, remove the patch if possible. For serious symptoms such as passing out or trouble breathing, give them naloxone if available, then call 911. If the person is awake and has no symptoms, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: slow/shallow breathing, slow heartbeat, coma.

Do not share this medication with others. Sharing it is against the law.

This medication has been prescribed for your current condition only. Do not use it later for another condition unless told to do so by your doctor. A different medication may be necessary in that case.

If you leave a patch on for more than 7 days, remove the patch and apply a new patch as soon as you remember. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not freeze. Keep all medications away from children and pets. See also Warning section.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed (see also How to Use section). For more details, read the Medication Guide, or consult your pharmacist or local waste disposal company.

Images

buprenorphine 10 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 20 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 15 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII 15

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 5 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 5 mcg/hour weekly transdermal patch

Color: beigeShape: squareImprint: Buprenorphine Transdermal System 5 mcg/hour

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 15 mcg/hour weekly transdermal patch

Color: beigeShape: rectangularImprint: Buprenorphine Transdermal System 15 mcg/hour

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 10 mcg/hour weekly transdermal patch

Color: beigeShape: rectangularImprint: Buprenorphine Transdermal System 10 mcg/hour

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 15 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII 15

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 20 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 20 mcg/hour weekly transdermal patch

Color: beigeShape: squareImprint: Buprenorphine Transdermal System 20 mcg/hour

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 5 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

buprenorphine 10 mcg/hour weekly transdermal patch

Color: tanShape: square (rounded corners)Imprint: Buprenorphine Transdermal System CIII

This medicine is a tan, square (rounded corners), transdermal system imprinted with “Buprenorphine Transdermal System CIII”.

Look up another drug

Find other drugs that treat your condition

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Transdermal Medications – StatPearls – NCBI Bookshelf

Samara Khan; Tariq Sharman.

Author Information and Affiliations

Last Update: February 6, 2023.

Continuing Education Activity

Transdermal drugs are medications used in managing and treating various conditions, including hypertension, motion sickness, pain, migraines, etc. This activity outlines the indications, action, and contraindications for transdermal drugs as a valuable agent in treating disorders when applicable. This activity will highlight the mechanism of action, adverse event profile, and other key factors (e.g., off-label uses, dosing, pharmacodynamics, pharmacokinetics, monitoring, relevant interactions) pertinent for members of the interprofessional team in the care of patients with conditions treated with transdermal drugs.

Objectives:

• Outline the mechanism of action of transdermal drug delivery with the various penetration enhancement techniques available.

• Summarize the risks of developing any adverse effects from transdermal drugs.

• Identify the methods of monitoring a transdermal patch 24 hours after administration to detect any toxicity caused by the transdermal drug delivery vessel or active substance.

• Explain the significance of communication at the interprofessional level to deliver quality care to patients using transdermal drug delivery techniques.

Access free multiple choice questions on this topic.

Indications

Transdermal drugs are a vast category of drugs defined as vessels for delivering drugs for a local or systemic mechanism of action via a specific dosing formulation. Transdermal drug delivery has become increasingly popular due to the significant advantages it carries. For example, transdermal drugs bypass the first-pass metabolism of the liver, protecting it from damage. Additionally, transdermal drugs decrease the risk of damage to the gastrointestinal system via the oral route, increase the likelihood of consistent patient use, and allow drug administration in a continuous stable-interval manner.[1][2] Transdermal administration also avoids the hepatic first-pass metabolism that affects orally administered drugs.

The fundamental principle of transdermal drug delivery relies on the ability of the drug to pass through the skin into the systemic circulation. Therefore, there are limited drugs that meet the criteria required to be able to bypass the skin. These criteria include having a low molecular weight (less than 600 g/mol), having the ability to pass through the epidermis, being absorbed by the blood vessels, and entering the circulation. Additionally, the active drug must be chemically and physically stable. The active substance must have a low daily dose for patient comfort and adhesive propensity. The skin should metabolize the drug. There have only been a limited number of successful transdermal drugs with such specific properties.[2][3]

Some indications that transdermal medications have been addressed since the 1970s include:

• Hypertension

• Local anesthesia

• Angina pectoris

• Motion sickness

• Pain

• Smoking control

• Migraine

• Major depression

• Parkinson disease

• Alzheimer disease

• ADHD

Transdermal administration is historically safe and effective when used as directed.

Mechanism of Action

The greatest challenge for the success of transdermal drug delivery is diffusing active substances through the barrier function of the many layers of the skin. The outermost layer of the skin, the stratum corneum, is the thickest layer containing numerous layers of keratin-heavy corneocytes. Additionally, the stratum corneum consists of two chemically different regions that need to be accounted for when creating transdermal drugs. There is an aqueous region at the outer surface of the keratin filaments and a lipid matrix between the filaments that active medications need to have the ability to diffuse through both to be successful.[4]

However, there have been recent advancements in the development of enhancement delivery methods for active drugs through the transdermal route. These methods are listed below:

• Microneedles: These are very small, painless needles that are either hollow or solid and filled with the desired drug. The microneedles pierce through the stratum corneum without causing a painful sensation. The advantages of this method are its painless nature and the ability to deliver compounds that have a higher molecular weight.

• Iontophoresis: The main force used to drive substances across the stratum corneum is the electrical driving force, where there is charged particle movement via electrophoresis. This way, a persistent low-voltage current enables the diffusion of substances across the stratum corneum. An electrical current can control drug delivery rate under the control of either a microprocessor or the patient.

• Thermal poration: The application of heat to the skin creates small pores in the skin for the easy diffusion of molecular substances across the stratum corneum.

• Electroporation: The application of a high electrical voltage to the stratum corneum also creates small pores for molecular substances to diffuse through the stratum corneum.

• Conventional enhancers: A chemical substance applied first to the skin to increase the permeability of the stratum corneum or change the thermodynamics of the active drug itself.

• Ultrasound: The application of sound waves to disrupt the stratum corneum and increase its permeability.[1][2][5][6]

Administration

Transdermal patches administration should follow a proper physical examination of patients and considerations of any associated comorbidities. The following steps are a general overview for administering a transdermal patch:

• Proper disinfecting and cleaning of skin where the patch is applied

• Application of patch in the desired area

• A follow-up appointment to ensure that the patient experiences no adverse skin reactions

• Proper adherence to the guidelines of the transdermal patch for future use

The administration of transdermal patches varies based on the drug administered via the patch.[7] However, certain steps generally apply to all transdermal patches:

1. The patient should clean and disinfect the area where they will apply the patch with clear water, patting the area until it is completely dry. They should avoid using any soaps, alcohols, lotions, or oils immediately before applying the patch.

2. They should open the pouch containing the patch and remove it from the pouch. Then peel off both parts of the protective liner from the back of the patch, being careful not to touch the adhesive side of the patch.

3. The patient should then immediately press the adhesive side of the patch onto their skin with the palm of their hand.

4. Hold or press the patch firmly for at least 30 seconds, ensuring the patch sticks well to the skin, especially at the edges.

5. If the patch does not adhere well or becomes loose following application, they can use first-aid tape to tape the edges to their skin. If the patch still fails to adhere well to the skin, they can try using see-through dressings but should not cover the patch with any other type of bandage or tape.

6. If a patch falls off before it is time to remove it, the patient must dispose of the patch properly and apply a new patch, following the same dosing interval as per the original patch. It is advisable to contact their clinician’s office or pharmacist in such cases.

7. Following the successful application of the patch, the patient should wash their hands with water immediately.

8. When it is time to change the patch, the patient will peel off the old patch and apply the new patch to a different area of the skin.

9. After removing the patch, the patient should fold it over with the adhesive sides together and dispose of it properly.

The patient should select different sites for consecutive applications to avoid skin irritation. Some patches are only meant to be worn for part of a day (e.g., 12 hours), while other patches are meant to be worn for several days. For example, fentanyl patches are worn for 72 hours and then removed and re-applied.

Patients need to understand that a removed patch can still contain enough medication to cause problems if they do not dispose of them properly. This is especially true if children can get a hold of them. Patches should not be used if they are damaged or torn, as this may cause a “dose dumping” phenomenon where the medication is dispensed more rapidly and at a greater dose than intended. If the patient has any questions about their transdermal patches, they should immediately contact their clinician or pharmacist.

Adverse Effects

The main adverse effects that can be caused by transdermal drug delivery are skin reactions. Transdermal patches are the most common method of delivery for active substances. Transdermal patches can irritate the skin and cause pruritis, burns, and redness of the surrounding area.[3] Additionally, allergic reactions are reported for all types of patches on the skin due to the active substance administered. The two most common skin reactions are irritant contact dermatitis and allergic contact dermatitis, both of which are usually caused by the drug or the patch, including adhesives and excipients.[8][9]

Obviously, using multiple patches when only one is indicated or leaving the path on longer than directed can lead to excessive medication dosing and even overdose.

Contraindications

Transdermal drug delivery is contraindicated in patients with[10]:

• Allergies to the active substance utilized in the transdermal patch

• Essential fatty acid deficiency

• Dry skin

• Psoriasis

• Ichthyosis

• Atopic dermatitis

• Increased ultraviolet radiation exposure

• Premature neonate

• Pregnant women (dependent on the drug administered)

Monitoring

The most significant issue associated with transdermal drug delivery is the likelihood of skin irritation caused by penetration enhancement techniques and the transdermal patch itself. Due to this, there have been models created to foresee the likelihood of skin irritation due to drug or vessel interaction using solubility and skin irritation studies using the PII test to detect redness or swelling 24 hours after administering the patch.[4][11]

Toxicity

The toxicity of the transdermal patch depends on the selected drug/active substance administered through the use of transdermal drug delivery and whether the patient properly follows administration directions.

Enhancing Healthcare Team Outcomes

Managing proper drug administration in healthcare requires interprofessional effort from various healthcare professionals such as clinicians, pharmacists, nurses, residents, etc. Numerous drug-related problems result in medication-related harm and low-quality healthcare for patients without appropriate regulation and administration techniques. To properly deliver a drug via transdermal patches, the following steps are necessary:

• Proper physical examination and updating the patient’s medical history by the prescribing clinician

• Consult with the pharmacist on the appropriate drug to be administered based on patient symptoms and history

• Consult with a clinician if there are any concerns about a transdermal patch

• If there is a life-threatening emergency related to the transdermal patch, the emergency department should be contacted immediately.

To enhance communication between healthcare professionals, techniques such as face-to-face interviews have proven to provide cohesiveness between pharmacists, primary care physicians, and surgical physicians for drug-related healthcare. It also includes reinforcement of patient counseling points to ensure proper administration and contacting the prescriber if it appears the patient is unable to perform self-administration properly. Ultimately, these techniques allow for an amplified patient-centered approach.[12][13] With interprofessional coordination and information sharing during patient care, transdermal medications can significantly benefit the appropriate patient population, resulting in improved medication adherence and better outcomes. [Level 5]

Review Questions

• Access free multiple choice questions on this topic.

• Comment on this article.

References

1.

Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol. 2008 Nov;26(11):1261-8. [PMC free article: PMC2700785] [PubMed: 18997767]

2.

Walter JR, Xu S. Therapeutic transdermal drug innovation from 2000 to 2014: current status and outlook. Drug Discov Today. 2015 Nov;20(11):1293-9. [PubMed: 26116094]

3.

Hupfeld S, Gravem H. [Transdermal therapeutic systems for drug administration]. Tidsskr Nor Laegeforen. 2009 Mar 12;129(6):532-3. [PubMed: 19282891]

4.

Benson HA. Transdermal drug delivery: penetration enhancement techniques. Curr Drug Deliv. 2005 Jan;2(1):23-33. [PubMed: 16305405]

5.

Tiwary AK, Sapra B, Jain S. Innovations in transdermal drug delivery: formulations and techniques. Recent Pat Drug Deliv Formul. 2007;1(1):23-36. [PubMed: 19075872]

6.

Subedi RK, Oh SY, Chun MK, Choi HK. Recent advances in transdermal drug delivery. Arch Pharm Res. 2010 Mar;33(3):339-51. [PubMed: 20361297]

7.

Leppert W, Malec-Milewska M, Zajaczkowska R, Wordliczek J. Transdermal and Topical Drug Administration in the Treatment of Pain. Molecules. 2018 Mar 17;23(3) [PMC free article: PMC6017304] [PubMed: 29562618]

8.

Pastore MN, Kalia YN, Horstmann M, Roberts MS. Transdermal patches: history, development and pharmacology. Br J Pharmacol. 2015 May;172(9):2179-209. [PMC free article: PMC4403087] [PubMed: 25560046]

9.

Romita P, Foti C, Calogiuri G, Cantore S, Ballini A, Dipalma G, Inchingolo F. Contact dermatitis due to transdermal therapeutic systems: a clinical update. Acta Biomed. 2018 Oct 26;90(1):5-10. [PMC free article: PMC6502158] [PubMed: 30889148]

10.

Kalia YN, Merino V, Guy RH. Transdermal drug delivery. Clinical aspects. Dermatol Clin. 1998 Apr;16(2):289-99. [PubMed: 9589202]

11.

Al Hanbali OA, Khan HMS, Sarfraz M, Arafat M, Ijaz S, Hameed A. Transdermal patches: Design and current approaches to painless drug delivery. Acta Pharm. 2019 Jun 01;69(2):197-215. [PubMed: 31259729]

12.

Foppe van Mil JW, Westerlund T, Brown L, Chen TF, Henman M, Hersberger K, McElnay J, Schulz M. Medical care and drug-related problems: Do doctors and pharmacists speak the same language? Int J Clin Pharm. 2016 Apr;38(2):191-4. [PubMed: 26797769]

13.

Foral PA, Anthone JM, Destache CJ, Vivekanandan R, Preheim LC, Gorby GL, Horne JM, Dobronski LA, Syed JJ, Mindru C, Ali MA, Ali KF, Neemann KA, Bittner MJ. Education and Communication in an Interprofessional Antimicrobial Stewardship Program. J Am Osteopath Assoc. 2016 Sep 01;116(9):588-93. [PubMed: 27571295]

Disclosure: Samara Khan declares no relevant financial relationships with ineligible companies.

Disclosure: Tariq Sharman declares no relevant financial relationships with ineligible companies.

Transdermal Therapeutic Systems (TTS)

The Transdermal Therapeutic System (TTS) is a promising dosage form that has been used by doctors and patients for about 20 years. TTCs have a number of undeniable advantages, especially for patients requiring long-term prophylaxis or treatment. However, despite this, so far not many drugs are available in this form. For example, in Russia there are only 12 such items. Registered patches are used in gynecology, rheumatology, neurology, oncology and in the treatment of nicotine addiction.

What is the convenience of TTS, what prevents them from being widely introduced into medical practice and what developments are underway, read in our article.

What is the transdermal therapeutic system?

TTC is a patch designed to introduce an active pharmacological agent into the bloodstream by diffusion through the skin. Depending on the structure, transdermal therapeutic systems are membrane and matrix.

B membrane (otherwise ravioli) – the drug in a liquid or gel state is in the tank and is gradually released through a porous material (membrane). Most often it is a polymer film. Outside the TTS is a protective outer layer. The first TTSs were performed using this technology; they are more voluminous in size and less convenient than matrix ones. For example, if the reservoir is accidentally damaged, the drug may be lost or, conversely, its increased absorption into the blood.

Matrix systems are simpler: under the outer protective material is a polymeric material with a drug evenly distributed in it (matrix). At the same time, the same material acts as an adhesive. Most of the existing TTCs are matrix. Membrane, based on the description in the GRLS, includes the Fendivia patch (the active ingredient is fentanyl).

What advantage does this dosage form have over the classical routes of administration?

TTS provides a continuous controlled flow of the drug into the blood for a long period (day, week) and allows you to maintain the concentration at a minimum level for the required pharmacological effect. At the same time, peak concentrations of the active substance do not occur in the blood, which occur during oral or injection administration. This reduces the risk of overdose, as well as toxic and negative side effects. Transdermal patches can be used when no other route of administration is possible, or their classical route of administration is less effective / safe (rapid destruction of the substance in the gastrointestinal tract, short half-life, narrow therapeutic corridor of action).

A prime example is fentanyl transdermal patches for the management of chronic pain (often in cancer patients). They may be given to a patient at home when other opioid analgesics have failed. There is currently no tablet form of fentanyl, and injections are available only in inpatient settings. From this point of view, fentanyl patches are unique.

Below you can see a table of all systems registered in the Russian Federation for transdermal drug transfer (according to GRLS).

Table (download).

The advantages of the dosage form include:

1. The form of choice when long-term painful injection therapy is required.
2. Form of choice when drugs are difficult to take orally or have a negative effect on the gastrointestinal tract.
3. No hepatic and gastrointestinal metabolism.
4. Constant uniform concentration of the drug in the blood at the minimum therapeutic level for a long time.
5. Relatively faster onset of action than oral formulations.
6. Lower risk of adverse reactions due to the absence of peak concentrations.
7. Patient convenience – reduces the frequency of dosing: no need to worry about the next dose, less risk of missing a dose.
8. Easy to cancel treatment by simply removing the patch.

TTC cons include:

1. Not suitable for certain skin conditions, skin reactions may occur.
2. Relatively higher price than oral and injectables.
3. A limited number of substances that can be administered with TTS due to their physical and chemical properties.
4. Only high-potency substances requiring low doses can be used in transdermal systems.
5. Slow development of effect compared to injections.

Patches can be improved

Transdermal therapeutic systems are a potentially very promising way to deliver drugs that require constant long-term administration (for example, insulin for diabetes mellitus, drugs for the treatment of cancer, mental illness, etc.). This route provides a painless, convenient, gradual delivery of the drug into the body with a reduced risk of side effects.

The barrier properties of the skin become a major barrier to the administration of many drugs via the transdermal system. For this reason, the amount of active pharmaceutical ingredients used is limited by a number of conditions. The drug molecule must be:

1. Low molecular weight (max. 500 Daltons)
2. Be lipophilic
3. Not charged

Current transdermal delivery systems include drug agents that meet these requirements. Nitroglycerin, Scopolamine, Testosterone, Clonidine, Nicotine, Estradiol, which have found their application in world practice, can be mentioned as examples of the first medicinal substances used in TTS. However, developments are being actively carried out to increase skin permeability and expand the possibilities of transdermal drug transport. Methods that facilitate the passage of molecules through the skin can be divided into chemical and physical.

The chemical method consists of adding penetrating chemicals to facilitate penetration of the therapeutic compound. These include ethyl alcohol, dimethyl sulfoxide, pyrrolidones, urea, fatty acids, transcutol, azone, isopropyl myristate. The chemical method is more suitable for relatively low molecular weight substances.

Electrical methods , such as iontophoresis, electroporation, electrophoresis are used to improve the transport ability of macromolecular compounds, most often peptides, nucleotides, proteins. As an example of TTS enhanced by iontophoresis, one can cite a transdermal system with lidocaine Lidosite® (not registered in the Russian Federation).

Microneedles. Delivery of drug compounds using microneedles is another highly promising method that allows hydrophilic macromolecules to pass through the protective barrier of the skin. Electrical methods in this case are not effective enough. The dosage form is an advanced hybrid of a transdermal patch and hypodermic needles. Micron-sized needles pierce the stratum corneum, bringing the drug to the emidermis or upper dermis, from where it can be freely absorbed into the bloodstream. At the same time, the person does not experience pain, since the needles do not touch the nerve endings. Skin damage is minimal and healing is fast, which reduces the risk of infection compared to conventional injections, and can also be self-administered by the patient. Microneedle TTS technology increases the potential of the dosage form for transdermal delivery of oligonucleotides used in gene therapy, insulin, interferons, vaccines. There are studies on the introduction of influenza vaccine, rabies vaccine, Desmopressin, Cyclosporine A, Insulin, Lidocaine, Meloxicam, antitumor compounds with the help of microneedles. In all cases, the high efficiency of this dosage form was confirmed.

Forward into the future

A large number of TTCs are in development and are on the way or about to enter the market. The list of active ingredients of transdermal systems is expanding.

• More recently, British scientists have created a transdermal patch with ibuprofen.
• The first and only patch for the treatment of adult schizophrenia SECUADO ® with the atypical antipsychotic Asenapine has been approved in the US.
• Using the technology of a microneedle patch, scientists are working on TTC with interferon, which is intended for cancer patients and people with viral hepatitis. According to calculations, the patch with microneedles should enter the Russian market in 7 years. At this stage, its effectiveness is being evaluated.
• A transdermal patch being developed by researchers at Queen’s University Belfast is designed to administer traditionally administered oral antibiotics. With the help of a patch dosage form, scientists hope to prevent the development of antibiotic resistance.
• Scientists from St. Petersburg are planning to implement an even more far-reaching technology: a patch with needles will be equipped with miniature electronic devices programmed to monitor the state of the human body. Depending on the results, the system will dose the administration of the drug. The smart patch is planned to be placed on the wrist, in appearance it will resemble a watch.

The market for alternative drug delivery systems is growing. It is predicted that by 2028 the global TTC market will reach $8 billion, which will be a 4% increase. Improvement in the methods of transdermal drug delivery will expand the possibilities of using this form in the prevention and treatment of various diseases.

Write in the comments if you have TTS in your arsenal of recommendations?

You can discuss the latest news with all your colleagues in Russia in chats:

• WhatsApp: https://chat. whatsapp.com/Izj3ZQ7aI36KK8e2dCjcm4
• Telegram: https://tglink.ru/joinchat/GWBPCkkLipQUnTbXrKqzGA
• VKontakte: https://vk.me/join/AJQ1dzabQRfHvl5Y2AOVUsgJ

The patch is a healthy alternative to the pill

03/24/2016

It’s no secret that many drugs have side effects. Especially often when using tablets and other dosage forms taken orally, the stomach suffers. Is there a healthy alternative to the pill? “Eat!” – say the pharmacists of “Klassika” and remind that in some cases traditional therapy can be successfully replaced by patches. One of the advantages is targeted action. Application transdermal drugs (TLP patches) can not only significantly reduce side effects, but also save your budget. Olga Shtreis, Leading Specialist in Pharmaceutical Activity of the Corporate Training Center of the Classica Pharmacy Chain, helped us to understand the issues of using modern TPP.

The history of the creation of transdermal (application) dosage forms has a long history. In the 5th-4th centuries BC, poultices of raw or boiled plants ground with wine or oil were used in medicine. In ancient times, ointments based on honey, oil, fresh lard, condensed juices and decoctions of plants in water or wine were also used.

Later came compresses, aromatic cakes. Almost all of these dosage forms have survived to this day. However, they do not regulate the rate of entry and concentration of biologically active compounds in the body and do not have a prolonged action. This task is designed to be solved by TLP – modern patches that allow long-term dosing of medicinal substances. This dosage form allows you to enter the drug into the systemic circulation according to a specific program. The active ingredients of the patch penetrate the human body through passive diffusion through the skin or mucous membranes. Before using transdermal drugs, consultation with your doctor is necessary, self-medication can lead to undesirable consequences.

In the online pharmacy “Classic” TLP are presented in a large assortment.

They can be divided into three groups:

1. patches containing drugs with anti-inflammatory and anesthetic activity, such as the Voltaren patch. It provides anti-inflammatory and analgesic action at the site of application, eliminating pain and reducing swelling associated with the inflammatory process.
2. patches containing therapeutic doses of, for example, nicotine. In the treatment of nicotine addiction, nicotine replacement therapy reduces the need for the number of cigarettes smoked, reduces the severity of withdrawal symptoms that occur with complete smoking cessation. Nicorette helps to reduce the number of cigarettes smoked by those who cannot or do not want to completely stop smoking.
3. patches containing hormonal preparations intended for the correction of conditions caused by the onset of menopause. For example, Klimara contains estriol for estrogen replacement therapy. The action of the substance is aimed at compensating for the deficiency of female sex hormones.