4S)-camphor

4S)-camphor Uses, Dosage, Side Effects, Food Interaction and all others data.

4S)-camphor, or L(-)-Camphor, is a stereoisomer of Camphor, a bicyclic monoterpene known to potentiate both heat and cold sensations . 4S)-camphor is not the naturally-occurring stereoisomer but displays similar TRPV channel affinity and current inhibition . Camphor is isolated from the wood of the camphor laurel tree, Cinnamomum camphora, and had a long history of medicinal use. It has been used as a nasal decongestant and cough suppressant, and has been topically applied due to its antipruritic, analgesic, and counterirritant properties . Camphor is a major active ingredient in over-the-counter balms and liniments supplied as topical analgesics by causing sensitization to heat and coolness to relieve minor muscle and joint pain .

Camphor exerts an analgesic action when applied topically by producing a warm sensation. It excites and desensitizes sensory nerves by activating heat-sensitive TRP vanilloid subtype 1 (TRPV1) and TRPV3 receptors. 4S)-camphor is reported to exert a weaker action on TRPV1 channels, which is thought to be a result of tachyphylaxis, which is the reduction of the response to multiple stimulations .

4S)-camphor
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
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Interaction With other Medicine
Contradiction
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Trade Name	4S)-camphor
Generic	(S)-camphor
(S)-camphor Other Names	(1S,4S)-camphor, l-camphor
Type
Formula	C₁₀H₁₆O
Weight	Average: 152.2334 Monoisotopic: 152.120115134
Protein binding	No pharmacokinetic data available.
Groups	Experimental
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Indicated for the temporary symptomatic relief of minor aches and pains of muscles and joints in topical analgesics.

4S)-camphor is also used to associated treatment for these conditions: Joint Pain, Soreness, Muscle

How 4S)-camphor works

TRPV3 cation channels are molecular sensors that play a role in nociception and thermosensation by inducing thermal sensation and heat-induced hyperalgesia . Camphor interacts with TRPV3 channels via pore-region cysteine residues , leading to channel activation and a rise in intracellular calcium levels. Camphor also activates TRPV1 and a TRPV1-like current in dorsal root ganglion (DRG) neurons but inhibits the ankyrin-repeat TRP 1 (TRPA1) channel expressed in most nociceptive DRG neurons, which is responsible for the detection of temperature . The precise role of TRPA1 current inhibition on the analgesic properties of camphor is unclear. Repeated stimulation by camphor leads to sensitization of the TRPV1 and TRPV3 channels, resulting in desensitization, or reduced channel response that likely leads to the analgesic effects of camphor . Camphor also activates cold-sensitive transient receptor potential melastatin 8 (TRPM8) and sensitizes cold-induced calcium transients, which explains the cooling effect of camphor following dermal application. Additionally, camphor was shown to inhibit the TRPM8 receptor response to menthol .

Toxicity

Oral LD50 and intraperitoneal LD50 in mouse were 1310 mg/kg and 3000 mg/kg, respectively . Subcutaneous LD50 in rat was 70 mg/kg .

The main target organs of camphor are the CNS and kidneys. Camphor is a CNS stimulant that may cause convulsions, depression, apnea, asystole, gastric irritation, colic, nausea, vomiting, diarrhea, anxiety, excitement, delirium, and severe post-convulsive coma . Camphor is also irritating to the eyes, skin and mucous membranes following dermal contact of high doses. Gastrointestinal irritation and CNS depression may occur at doses over 10 mg/kg while as little as 1 g has been fatal in infants, and death has been reported with doses of 50 mg/kg or more . There is no known antidote for camphor intoxication, thus gastrointestinal decontamination via activated charcoal is generally recommended for oral camphor overdose .

Volume of Distribution

Volume of distribution of camphor is 2 to 4 L/kg . Camphor and its metabolites are relatively fat-soluble thus may accumulate in adipose and other tissues . Camphor ingested by mothers was present in amnionic fluid, cord and fetal blood and fetal brain, liver and kidneys .

Elimination Route

Absorption of camphor in the mucous membranes and the gastrointestinal tract is rapid, and peak concentration following oral ingestion occurs within 5 to 90 minutes .