Capsaicin

Authors: Prof. Dr. med. Peter Altmeyer, Prof. Dr. med. Martina Bacharach-Buhles

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Last updated on: 24.02.2024

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Synonym(s)

Shaking mixture Capsaicin containing 001% capsaicin

Definition
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Capsaicin is a heat-stable alkaloid (vanillylamide) obtained from paprika (see also cayenne pepper extract; see also Capsici fructus acer), which only causes a heat or pungency stimulus (see below pungent substances) in mammals by acting on specific receptors, for example when eating paprika or chili peppers. In contrast to antihistamines, the pungent substance capsaicin can also be used topically for non-histamine-induced pruritus.

Pharmacodynamics (Effect)
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Capsaicin is absorbed through the skin and produces a feeling of warmth (antagonist of menthol) as well as capillary dilation. The substance has an antiphlogistic and anesthetic effect. There is evidence that the synapses of the peripheral nerves are emptied.

Binding to a calcineurin receptor (see capsaicin receptor. S.a menthol receptor) causes a type of "desensitization" of sensory nerve fibres and thus interrupts the transmission of cutaneous pruritus and pain stimuli.

Indication
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Pruritus, pain, e.g. in zoster neuralgia (Reimann S et al. 2000/b: Reimann S et al. 2000)

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With regard to atopic dermatitis, significant itching relief has been reported in experimental studies312 and case series313 . However, the practical implementation in treatment and the top-up dosage are difficult due to the initially high release of neuropeptides that trigger discomfort (Weisshaar E et al. (1998) Effect of topical capsaicin on the cutaneous reactions and itching to histamine in atopic eczema compared to healthy skin. Arch Dermatol Res. Jun 290:306-311 No controlled study on the indication "atopic dermatitis" has been published to date

Dosage and method of use
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Apply cream several times a day, approx. 3-4 times, to the itchy, burning area. Slowly start the therapy, patients must be informed about the short-term burning at the treated area (stops after about 3-5 days).

Standard concentration
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0.01-0.5% in creams or shaking mixtures.

Notice! Avoid contact with mucous membranes and eyes! Capsaicin burns on open areas!

Undesirable effects
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Skin irritation, burning, erythema, urticaria, sensitization.

Contraindication
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Hypersensitivity to paprika preparations.

Recipe(s)
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Capsaicin shaking mixture 0.01%

Notes on the formulation: Capsaicinoids DAC are not available as a formulation substance. Capsaicin USP, which is currently available, can be used as an alternative. It can be used in the same concentration as capsaicinoids DAC. Although the composition is not completely identical, this should not be therapeutically relevant. It can also be used to produce the propylene glycol concentrate in accordance with NRF specification S.49., which is then further processed into creams, e.g. NRF 11.125. Capsaicin cream, hydrophilic 0.025/0.05; 0.075 or Capsaicin cream, hydrophilic 0.1% (NRF 11.125.).

Cave! Formulations are considerably more expensive than ready-to-use preparations!

Preparations
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Capsamol, Jucurba Capsicum Pain Emulsion, ABC Local Pain Therapy Heat Cream 750 µg/g (50g), Thermazet®

Literature
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  1. Carnevale V et al. (2016) A Target for Rational Drug Design. Pharmaceuticals (Basel) 9. pii: E52.
  2. Fernandes ES et al. (2016) Capsaicin and Its Role in Chronic Diseases. Adv Exp Med Biol 929:91-125.
  3. Laklouk M et al. (2016) Profile of the capsaicin 8% patch for the management of neuropathic pain associated with postherpetic neuralgia: safety, efficacy, and patient acceptability. Patient Prefer Adherence 10:1913-1918.
  4. Reimann S et al. (2000) Effect of topical capsaicin on the cutaneous reactions and itching to histamine in atopic eczema compared to healthy skin. Arch Dermatol Res. Jun 290:306-311.

  5. Reimann S et al. (2000) Topical administration of capsaicin in dermatology for treatment of itching and pain. Dermatology 51:164-172.

  6. Simpson DM et al.(2016) Capsaicin 8% Patch in Painful Diabetic Peripheral Neuropathy: A Randomized, Double-Blind, Place o-Controlled Study. J Pain pii: S1526-5900
  7. Ständer S et al. (2006) Diagnostic and therapeutic procedures in chronic pruritis. J Dtsch Dermatol Ges 4: 350-370
  8. Takahashi N et al. (2014) Epithelial TRPV1 Signaling Accelerates Gingival Epithelial Cell Proliferation. J Dent Res 93:1141-1147
  9. Weisshaar E et al. (1998) Effect of topical capsaicin on the cutaneous reactions and itching to histamine in atopic eczema compared to healthy skin. Arch Dermatol Res. Jun 290:306-311
  10. Zis P et al. (2016) Effectiveness and Impact of Capsaicin 8% Patch on Quality of Life in Patients with Lumbosacral Pain: An Open-label Study. Pain Physician E1049-53.