Capsaicin (capsaicin)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Capsaicin is a transient receptor potential vanilloid 1 (TRPV1) receptor agonist.
Capsaicin, a naturally occurring alkaloid found in hot peppers and related plants, is a transient receptor potential vanilloid 1 (TRPV1) receptor agonist that acts as a chemoneurolytic agent. TRPV1 is an ion channel-receptor complex primarily expressed in peripheral sensory neurons, but also found in the trigeminal ganglia and dorsal root. TRPV1 receptors are upregulated during chronic pain states, reducing the stimulation threshold and increasing pain perception.
Activation of these receptors results in the perception of pain, burning, itching, and stinging sensations. The effects of capsaicin on pain modulation are multifactorial and vary based on concentration. Low concentrations of capsaicin produce transient analgesia by activating TRPV1, causing calcium influx and subsequent inactivation of voltage-dependent sodium channels, voltage-dependent calcium channels, and a mechanosensitive ion channel; these actions lead to short-term defunctionalization of nociceptor terminals.
High concentrations of capsaicin lead to long-term defunctionalization mediated by the ablation of TRPV1-expressing afferent nerve terminals, resulting in long-lasting analgesia for several months. Following topical application, capsaicin causes enhanced sensitivity followed by a period of reduced sensitivity; after repeated applications, persistent desensitization occurs. Initial binding of capsaicin to TRPV1 receptors in the skin results in depolarization and production of action potentials perceived as itching, pricking, or burning sensations.
This is followed by pain relief, which is thought to be mediated by a reduction in TRPV1-expressing nociceptive nerve endings.
Capsaicin 8% is a topical system consisting of a silicon adhesive mixture with a high concentration of capsaicin (640 mcg/cm2) dissolved in diethylene glycol monoethyl ether. When applied topically, the matrix technology in the delivery system forces diffusion of high-concentration capsaicin into the epidermis and dermis where it activates TRPV1 receptors and exerts its therapeutic effect.
Following topical application, capsaicin is rapidly diffused into epidermal layers of the skin with sufficient cutaneous bioavailability observed in both thick and thin skin. Systemic absorption is negligible since the drug does not penetrate deep into dermal layers of the skin. Following a 60-minute application of a capsaicin 8% topical system in patients with PHN, transient, low (<5 ng/mL) systemic exposure to the drug was observed in about one-third of patients.
The highest plasma concentration detected was 4.6 ng/mL and occurred immediately after removal of the topical system. Most quantifiable levels were observed at the time of removal and were below the limit of quantitation 3 to 6 hours after removal of the topical system. No detectable levels of metabolites were observed in any subject.
Capsaicin is used topically for the treatment of pain. Capsaicin 8% topical system is FDA-labeled for the treatment of neuropathic pain associated with postherpetic neuralgia (PHN) and for the treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPN) of the feet. Capsaicin is also available in various over-the-counter (OTC) topical preparations for the treatment of pain due to diabetic neuropathy, herpes zoster, or arthritis; preparations available for OTC use contain lower concentrations of capsaicin (e.g., 0.025-0.15%) than the capsaicin 8% topical system.
Generic name: capsaicin
Pronunciation: (kap-SAY-i-sin)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Capsaicin
Indications
The following indications are listed for Capsaicin:
- Arthritic Pain
- Back Pain
- Sprains And Strains
Also known as: Sprains And Joint Or Muscle Strains, Sprains And Muscle Or Joint Strains, Sprains And Muscle Strains.
Dosing
No dosing information is available for this tab.
Capsaicin 8% is commercially available as a single-use topical system stored in a foil pouch; each topical system contains 179 mg of capsaicin. Apply capsaicin 8% topical system to affected areas of the skin. The topical system should be applied by a healthcare professional in a controlled setting to avoid severe irritation to the eyes, mucous membranes, respiratory, and skin from unintended exposure.
Use nitrile gloves when handling the topical system; do not use latex gloves. Use of a face mask and protective glasses is also advised for healthcare professionals.
Store capsaicin 8% topical system at 20-25degreesC (excursions permitted between 15-30degreesC) in its sealed pouch until immediately before use. Inspect the pouch prior to use; do not use if the pouch has been damaged or torn.
Apply the topical system to dry, intact (unbroken) skin; do not apply to the face, eyes, mouth, nose, or scalp. A physician or healthcare professional should identify and mark the treatment area (areas of hypersensitivity and allodynia). In patients with diabetic neuropathy, the topical system may be wrapped around the dorsal, lateral, and plantar surfaces of each foot to completely cover the treatment area. If necessary, hair around the treatment area can be clipped to promote adhesion of the topical system; do not shave the hair. The topical system may be cut to match the size and shape of the treatment area before removing the protective release liner. Up to 4 topical systems may be used during a single treatment session to cover larger areas. Once the topical system is applied, leave on for 60 minutes (for the treatment of postherpetic neuralgia (PHN)) or 30 minutes (for the treatment of DPN of the feet). A dressing such as rolled gauze may be used to cover the topical system to ensure that it maintains contact with the treatment area.
At the end of the treatment session, use nitrile gloves to remove the topical system by gently and slowly rolling the topical system inward. After removal, apply the manufacturer-supplied cleansing gel to the treatment area and leave on for at least 1 minute. Remove the gel with a dry wipe and gently wash the area with mild soap and water; dry thoroughly. The treatment area may be sensitive for a few days to heat (e.g., hot showers/baths, direct sunlight, vigorous exercise).
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No clinical drug interaction studies have been performed with capsaicin 8% topical system. In vitro studies indicate that the drug does not inhibit or induce cytochrome P-450 (CYP) enzymes at concentrations that far exceed those in blood concentrations of patients receiving capsaicin 8% topical system; therefore, drug interactions with systemic medications are unlikely.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions (>=5%) reported with capsaicin 8% topical system in clinical studies were application site erythema, application site pain, and application site pruritus.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and effectiveness of capsaicin 8% topical system in pediatric patients younger than 18 years of age have not been established.
Maternal use of capsaicin 8% topical system is not expected to result in fetal exposure; systemic absorption of the drug following topical administration is negligible. In animal reproductive studies, no evidence of malformations were observed when capsaicin was administered daily by the topical route to pregnant rats and rabbits during the period of organogenesis at doses of up to 11- and 37-times, respectively, the maximum recommended human dose (MRHD) at 716 mg capsaicin per day (4 topical systems containing 179 mg/topical system). In a peri- and postnatal development study, no adverse effects were observed when capsaicin was administered daily by the topical route to rats during implantation to weaning at doses of up to 11-times the MRHD.
Breastfeeding is not expected to result in fetal exposure of capsaicin; systemic absorption from topical application of capsaicin 8% topical system is negligible. There are no data on the effects of capsaicin on human milk production.
To minimize potential direct exposure of capsaicin to the breastfed infant, avoid applying the topical system directly to the nipple and areola. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for capsaicin and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition.
No dosage adjustments are required in geriatric patients.
In controlled clinical trials of capsaicin 8% topical system in patients with postherpetic neuralgia, 75% of patients were 65 years of age and older and 43% of patients were 75 years of age and older. The safety and effectiveness were similar in geriatric patients and younger patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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