Akarpine - General Information
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Akarpine is used as a miotic and in the treatment of glaucoma.
Pharmacology of Akarpine
Akarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Akarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Akarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.
Akarpine for patients
Patients should be informed that pilocarpine may cause visual disturbances, especially at night, that could impair their ability to drive safely.
If a patient sweats excessively while taking pilocarpine hydrochloride and cannot drink enough liquid, the patient should consult a physician. Dehydration may develop.
Pilocarpine should be administered with caution to patients taking beta adrenergic antagonists because of the possibility of conduction disturbances. Drugs with parasympathomimetic effects administered concurrently with pilocarpine would be expected to result in additive pharmacologic effects. Pilocarpine might antagonize the anticholinergic effects of drugs used concomitantly. These effects should be considered when anticholinergic properties may be contributing to the therapeutic effect of concomitant medication (e.g., atropine, inhaled ipratropium).
While no formal drug interaction studies have been performed, the following concomitant drugs were used in at least 10% of patients in either or both Sjögrens efficacy studies: acetylsalicylic acid, artificial tears, calcium, conjugated estrogens, hydroxychloroquine sulfate, ibuprofen, levothyroxine sodium, medroxyprogesterone acetate, methotrexate, multivitamins, naproxen, omeprazole, paracetamol, and prednisone.
SALAGEN Tablets are contraindicated in patients with uncontrolled asthma, known hypersensitivity to pilocarpine, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure) glaucoma.
Additional information about Akarpine
Akarpine Indication: For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.
Mechanism Of Action: Akarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Pilocarpine
Synonyms: Pilocarpine chloride; Pilocarpine HCl; Pilocarpine hydrochloride; Pilocarpine monohydrochloride; Pilocarpine muriate; Pilokarpin monohydrochloride; Pilokarpin; Pilocarpin; Spersacarpine hydrochloride; Spersacarpine; Adsorbocarpine; Beta-pilocarpine hydrochloride
Drug Category: Cholinergic Agents; Muscarinic Agonists; Miotics
Drug Type: Small Molecule; Approved
Other Brand Names containing Pilocarpine: Akarpine; Almocarpine; Ami-Pilo; Amistura P; Epicar; Isopto Carpine; Isoptocarpine; Mi-Pilo; Mi-Pilo Ophth Sol; Minims Pilocarpine; Miocarpine; Mistura P; Ocu-Carpine; Ocusert P 20; Ocusert Pilo; Ocusert Pilo-20; Ocusert Pilo-40; P.V. Carpine Liquifilm; Pilagan; Pilocar; Pilocar SMP; Pilocarpal; Pilocarpol; Pilocel; Pilokarpol; Pilomiotin; Pilopine HS; Piloptic-1; Piloptic-1/2; Piloptic-2; Piloptic-3; Piloptic-4; Piloptic-6; Pilostat; Pilovisc; Salagen; Sno Pilo; Syncarpine;
Absorption: There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Possibly occurs at the neuronal synapses and in the plasma
Half Life: 0.76 hours
Dosage Forms of Akarpine: Solution / drops Oral
Chemical IUPAC Name: (3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one
Chemical Formula: C11H16N2O2
Pilocarpine on Wikipedia: http://en.wikipedia.org/wiki/Pilocarpine
Organisms Affected: Humans and other mammals