QUTENZA® (capsaicin)

QUTENZA® (capsaicin) topical system

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QUTENZA® (capsaicin)

QUTENZA (capsaicin) 8% topical system contains capsaicin in a localized dermal delivery system. The capsaicin in QUTENZA is a synthetic equivalent of the naturally occurring compound found in chili peppers. Capsaicin is soluble in alcohol, acetone, and ethyl acetate and very slightly soluble in water.

QUTENZA is a single-use topical system stored in a foil pouch. Each QUTENZA is 14 cm x 20 cm (280 cm2 ) and consists of a polyester backing film coated with a drug-containing silicone adhesive mixture and covered with a removable polyester release liner.

The backing film is imprinted with “capsaicin 8%”. Each QUTENZA contains a total of 179 mg of capsaicin (8% in adhesive, 80 mg per gram of adhesive) or 640 micrograms (mcg) of capsaicin per square cm of topical system.

The empirical formula is C18H27NO3, with a molecular weight of 305.42. The chemical compound capsaicin [(E)-8-methyl-N-vanillyl-6-nonenamide] is an activating ligand for transient receptor potential vanilloid 1 receptor (TRPV1).

QUTENZA is supplied with a Cleansing Gel which is used to remove residual capsaicin from the skin after treatment. Cleansing Gel consists of the following ingredients: butylated hydroxyanisole, carbomer copolymer, edetate disodium, polyethylene glycol, purified water, and sodium hydroxide.

Indications and usage

QUTENZA is a TRPV1 channel agonist indicated for the treatment of neuropathic pain associated with postherpetic neuralgia (PHN) and neuropathic pain associated with diabetic peripheral neuropathy (DPN) of the feet.

Mechanism of Action

Capsaicin is an agonist for the transient receptor potential vanilloid 1 receptor (TRPV1), which is an ion channel-receptor complex expressed on nociceptive nerve fibers in the skin. Topical administration of capsaicin causes an initial enhanced stimulation of the TRPV1-expressing cutaneous nociceptors that may be associated with painful sensations. This is followed by pain relief thought to be mediated by a reduction in TRPV1-expressing nociceptive nerve endings. Over the course of several months, there may be a gradual re-emergence of painful neuropathy thought to be due to TRPV1 nerve fiber reinnervation of the treated area.

Pharmacokinetics

Pharmacokinetic data in humans showed transient, low (<5 ng/mL) systemic exposure to capsaicin in about one-third of PHN patients following 60-minute applications of QUTENZA. The highest plasma concentration of capsaicin detected was 4.6 ng/mL and occurred immediately after QUTENZA removal. Most quantifiable levels were observed at the time of QUTENZA removal and were below the limit of quantitation 3 to 6 hours after QUTENZA removal. No detectable levels of metabolites were observed in any subject.

Dosage and administration

  • Only physicians or health care professionals under the close supervision of a physician are to administer QUTENZA.
  • Administer QUTENZA in a well-ventilated treatment area.
  • Wear nitrile (not latex) gloves when handling QUTENZA and when cleaning treatment areas.
  • Use of a face mask and protective glasses is advisable for healthcare professionals.
  • Do not use QUTENZA on broken skin.
  • PHN: Apply up to four topical systems for 60 minutes.
  • DPN: Apply up to four topical systems for 30 minutes on the feet.
  • Repeat every 3 months or as warranted by the return of pain (not more frequently than every three months).

Warning and precautions

Unintended exposure to capsaicin can cause severe irritation of eyes, mucous membranes, respiratory tract, and skin in healthcare professionals, patients, and others. Ensure that the recommended procedures and protective measures are used when administering QUTENZA

Eye and Mucous Membrane Exposure:

  • For healthcare professionals: Wear nitrile gloves when administering QUTENZA and avoid unnecessary contact with items in the room, including items that the patient may later have contact with, such as horizontal surfaces and bedsheets. Use of a face mask and protective glasses is advisable.
  • Do not apply QUTENZA to the patient’s face, eyes, mouth, nose, or scalp to avoid risk of exposure to eyes or mucous membranes.
  • Accidental exposure to the eyes and mucous membranes can occur from touching QUTENZA or items exposed to capsaicin and then touching the eyes and mucous membranes.
  • If irritation of eyes or mucous membranes occurs, flush eyes and mucous membranes with cool water. Remove the affected individual (healthcare professional or patient) from the vicinity of QUTENZA.

Respiratory Tract Exposure:

  • Aerosolization of capsaicin can occur upon rapid removal of QUTENZA. Therefore, remove QUTENZA gently and slowly by rolling the adhesive side inward.
  • Inhalation of airborne capsaicin can result in coughing or sneezing. Administer QUTENZA in a wellventilated treatment area. Provide supportive medical care if shortness of breath develops. If irritation of airways occurs, remove the affected individual (healthcare professional or patient) from the vicinity of QUTENZA. If respiratory irritation worsens or does not resolve, do not re-expose the affected healthcare professional or patient to QUTENZA

Skin Exposure:

  • If skin not intended to be treated is exposed to QUTENZA, apply Cleansing Gel for one minute and wipe off with dry gauze. After the Cleansing Gel has been wiped off, wash the area with soap and water.

Thoroughly clean all areas that had contact with QUTENZA and properly dispose of QUTENZA, associated packaging, Cleansing Gel, gloves, and other treatment materials in accordance with local biomedical waste procedures

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Application-Associated Pain: Even following use of a local anesthetic prior to administration of QUTENZA, patients may experience substantial procedural pain and burning upon application of QUTENZA and following removal of QUTENZA. Prepare to treat acute pain during and following the application procedure with local cooling (such as an ice pack) and/or appropriate analgesic medication.

Increase in Blood Pressure: In clinical trials, transient increases in blood pressure occurred during or shortly after exposure to QUTENZA. The changes averaged less than 10 mm Hg, although some patients had greater increases and these changes lasted for approximately two hours after QUTENZA removal. Increases in blood pressure were unrelated to the pretreatment blood pressure but were related to treatment-related increases in pain. Monitor blood pressure periodically during and following the treatment procedure and provide adequate support for treatment-related pain.

Sensory Function: Reductions in sensory function have been reported following administration of QUTENZA. Decreases in sensory functions are generally minor and temporary (including to thermal and other harmful stimuli). All patients with pre-existing sensory deficits should be clinically assessed for signs of sensory deterioration or loss prior to each application of QUTENZA. If sensory deterioration or loss is detected or pre-existing sensory deficit worsens, continued use of QUTENZA treatment should be reconsidered.

Use in specific populations

Pregnancy: Capsaicin is negligibly absorbed systemically following topical administration of QUTENZA, and maternal use is not expected to result in the fetal exposure to QUTENZA. 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) of QUTENZA 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

Lactation: Capsaicin is negligibly absorbed systemically by the mother following topical administration of QUTENZA, and breastfeeding is not expected to result in exposure of the infant to QUTENZA. There are no data on the effects of capsaicin on milk production. To minimize potential direct exposure of QUTENZA to the breastfed infant, avoid applying QUTENZA directly to the nipple and areola.

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for QUTENZA and any potential adverse effects on the breastfed infant from QUTENZA or from the underlying maternal condition.

Females and Males of Reproductive Potential: In a fertility and reproductive toxicology study, administration of QUTENZA at 13-times the MRHD to male rats for 3 hours/day for 49 days resulted in a statistically significant reduction in the number and percent of motile sperm; however, these reductions did not adversely affect fertility. As this animal model has a large excess of sperm-generating capacity relative to the threshold necessary for fertilization, the lack of an effect on fertility in this species is of unknown clinical significance for males of reproductive potential treated with the MRHD.

Pediatric Use: The safety and effectiveness of QUTENZA in patients younger than 18 years of age have not been studied.

Geriatric Use: In controlled clinical trials of QUTENZA in neuropathic pain associated with postherpetic neuralgia, 75% of patients were 65 years and older and 43% of patients were 75 years and older. The safety and effectiveness were similar in geriatric patients and younger patients. No dose adjustments are required in geriatric patients

Overdosage

There is no clinical experience with QUTENZA overdose in humans.

There is no specific antidote for overdose with capsaicin. In case of suspected overdose, remove QUTENZA gently, apply Cleansing Gel for one minute, wipe off with dry gauze, and gently wash the area with soap and water. Use supportive measures and treat symptoms as clinically warranted.

Storage

Store carton between 20°C to 25°C (68°F to 77°F). Excursions between 15°C and 30°C (59°F and 86°F) are allowed. Keep QUTENZA in the sealed pouch until immediately before use.

Handling and Disposal

Unintended exposure to capsaicin can cause severe irritation of eyes, skin, respiratory tract, and mucous membranes. Wear nitrile (not latex) gloves while administering QUTENZA. Use of a face mask and protective glasses is advisable. Immediately after use, dispose of used and unused QUTENZA, QUTENZA clippings, associated packaging, Cleansing Gel, and all other potentially contaminated treatment supplies in accordance with local biomedical waste procedures

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