Capsaicin

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

Last updated on: 18.01.2022

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 in mammals causes a heat or pungency stimulus (see pungent substances below) by acting on specific receptors, for example when eating paprika or chilli peppers. In contrast to antihistamines, the pungent substance capsaicin can also be applied topically in case of non-histamine-induced pruritus.

Pharmacodynamics (Effect)
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Capsaicin is absorbed through the skin and generates a feeling of warmth ( menthol antagonist) in addition to capillary dilation. The substance has an antiphlogistic and anaesthetic effect. Evidence of emptying of the synapses of the peripheral nerves can be found.

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

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Indication
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Pruritus, pain, e.g. in zoster neuralgia.

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%.

Capsaicin cream, hydrophilic 0.025/0.05; 0.075 or 0.1% (NRF 11.125.)

Caveat. Formulations are much 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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Carnevale V et al. (2016) A Target for Rational Drug Design. Pharmaceuticals (Basel) 9. pii: E52.
Fernandes ES et al (2016) Capsaicin and Its Role in Chronic Diseases. Adv Exp Med Biol 929:91-125.
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.
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.
Ständer S et al (2006) Diagnostic and therapeutic procedures in chronic pruritis. J Dtsch Dermatol Ges 4: 350-370
Takahashi N et al (2014) Epithelial TRPV1 signaling accelerates gingival epithelial cell proliferation. J Dent Res 93:1141-1147
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.
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