Crisugabalin + probenecid + cimetidine

This entry describes a combination of three distinct pharmaceutical agents: Crisugabalin (also known as HSK16149), probenecid, and cimetidine. Crisugabalin is a novel GABA analogue and a selective ligand of the α2δ subunit of voltage-gated calcium channels, primarily α2δ-1. Its mechanism involves reducing calcium ion influx in the central nervous system, thereby decreasing the release of excitatory neurotransmitters like glutamate and norepinephrine. It is developed by Haisco Pharmaceutical Group Co., Ltd. and is approved in China for the treatment of diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). Probenecid is a uricosuric agent that functions by competitively inhibiting the reabsorption of uric acid via organic anion transporter 1 (OAT1) and urate transporter 1 (URAT1) in the renal tubules, leading to increased uric acid excretion. It also inhibits the renal excretion of certain antibiotics, such as penicillin and cephalosporins, thereby increasing their plasma concentrations. Probenecid is approved for treating gout and hyperuricemia, and as an adjunct to antibiotic therapy. Cimetidine is a histamine H2 receptor antagonist that competitively blocks histamine from stimulating H2-receptors on gastric parietal cells, which reduces gastric acid secretion. Developed by Smith Kline & French, it is approved for conditions like heartburn, peptic ulcers, and gastroesophageal reflux disease. Cimetidine is also a potent inhibitor of several cytochrome P450 (CYP) enzymes (e.g., CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4). The co-administration of these three drugs would involve significant pharmacokinetic considerations due to probenecid's inhibition of renal transporters and cimetidine's broad CYP inhibition, potentially altering the metabolism and excretion of Crisugabalin or other co-administered drugs.

Brand names

Simei NingProbalanBenemidTagametTagamet HBAcid ReducerMajor Acid Reducer