Akarpine
Akarpine Uses, Dosage, Side Effects, Food Interaction and all others data.
Akarpine Hydrochloride directly stimulates cholinergic receptors. It produces contraction of the iris sphincter muscle, resulting in pupillary constriction (miosis); constriction of the ciliary muscle, resulting in increased accommodation; and reduction in intraocular pressure associated with an increase in the outflow and a decrease in the inflow of aqueous humor. In chronic open angle glaucoma, the exact mechanism by which miotics lower intraocular pressure is not exactly known; however, contraction of the ciliary muscle apparently opens the intertrabecular spaces and facilitates aqueous humor outflow. There is also a decrease in the rate of inflow of aqueous humor. In angle-closure glaucoma, constriction of the pupil apparently pulls the iris away from the trabeculum, thereby relieving blockage of the trabecular meshwork.
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.
| Trade Name | Akarpine |
| Availability | Prescription only |
| Generic | Pilocarpine |
| Pilocarpine Other Names | Pilocarpina, Pilocarpine |
| Related Drugs | glycerin topical, Salagen, Biotene Mouthwash, XyliMelts, SalivaMAX |
| Weight | 1%, 2%, 4% |
| Type | Ophthalmic solution |
| Formula | C11H16N2O2 |
| Weight | Average: 208.2569 Monoisotopic: 208.121177766 |
| Groups | Approved, Investigational |
| Therapeutic Class | Drugs affecting exocrine secretions |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Akarpine is used for chronic open angle glaucoma, acute or chronic narrow angle glaucoma, suspected glaucoma and ocular hypertension.
Akarpine is also used to associated treatment for these conditions: Dry Mouth, Glaucoma, Closed-Angle, Glaucoma, Narrow Angle, Increased Intra Ocular Pressure (IOP), Ocular Hypertension, Open Angle Glaucoma (OAG), Open-angle Glaucoma (OAG), Acute Angle closure glaucoma, Chronic open-angle glaucoma
How Akarpine works
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.
Dosage
Akarpine dosage
Instill 1 drop 2-4 times daily. To minimize systemic absorption of the active ingredient of the eye drops, pressure should be applied for one minute on the tear duct after application.
Side Effects
Common: Temporary blurred vision, burning, stinging, redness, watering of the eyes, decrease in night vision, eye irritation, headache.
Rare: Eye pain, increased sweating, muscle tremors, nausea, vomiting, diarrhea, watering of the mouth, troubled breathing or wheezing.
Precaution
If blurred vision or changes in near or far sight occur, especially at night, patients should exercise caution when involved in night driving or hazardous work in poor light. It is recommended that intraocular pressure measurements be performed regularly during therapy.
Interaction
Belladonna alkaloids or cyclopentolate used ophthalmically may interfere with the miotic effects of pilocarpine and may have their own mydriatic effects dampened. This latter may be used to therapeutic advantage.
Food Interaction
- Take with or without food. The Cmax of pilocarpine is slightly reduced when taken with food.
Akarpine Hypertension interaction
[Major] The use of cholinergic agonists, such as bethanechol and pilocarpine, is contraindicated in patients with pronounced bradycardia, hypotension
Akarpine Drug Interaction
Moderate: metoprololUnknown: amphetamine / dextroamphetamine, aspirin, diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, cyclobenzaprine, pregabalin, esomeprazole, hydroxychloroquine, cyclosporine ophthalmic, montelukast, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, ergocalciferol, cholecalciferol, ondansetron, cetirizine
Akarpine Disease Interaction
Major: bronchospasm, cardiac dysfunction, GI/bladder neck obstruction, hyperthyroidism, parkinsonism, seizure disorders, glaucomaModerate: cholelithiasis, nephrolithiasis
Elimination Route
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
Half Life
0.76 hours
Pregnancy & Breastfeeding use
Safe use during pregnancy has not been established. Problems in human pregnancy have not been documented. However, ophthalmic Akarpine is systemically absorbed.
Contraindication
Hypersensitivity to any ingredient including excipients. Conditions where pupillary constriction is undesirable (e.g. acute iritis). Retinal detachment; past history of retinal detachment or conditions that predispose to retinal detachment.
Acute Overdose
Dilution with water and other fluids is the usual response to accidental or deliberate overdose.
Storage Condition
Store at room temperature and protect from light. It is desirable that the contents should not be used more than 4 weeks after first opening of the bottle.
Innovators Monograph
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