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Composition w/v |
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Pilocarpine Nitrate IP |
2% |
Chlorbutol IP |
0.5% |
(As Preservative) |
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Sterile buffered base |
q.s. |
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Clinical Pharmacology |
Pilocarpine nitrate 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
- Reduction in intraocular pressure associated with an increase in the outflow and a decrease in the inflow of aqueous humour. |
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Pharmacokinetics |
Miosis (pupillary constriction) occurs within 10 to 30 minutes and lasts 4 to 8 hours. Intraocular pressure starts decreasing within 75 minutes and persists for 4 to 6 hours. Page 1 of 3 Page 2 of 3 Following systemic absorption pilocarpine undergoes biotransformation which is thought to occur at the neural synapses and in the plasma. Elimination occurs in the urine, as unchanged pilocarpine and its minimally active or inactive degradation products, such as pilocarpic acid. |
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Indication |
Miosis induction, postoperative or Miosis induction, following ophthalmoscopy—Pilocarpine (hydrochloride or nitrate) ophthalmic solution is indicated to produce miosis in order to counteract the effects of cycloplegics and mydriatics following surgery or ophthalmoscopic examination. |
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Dosage & Administration |
1 to 2 drops of Carpinol 2% should be instilled in the affected eye[s]. Two to four times a day. |
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Warnings |
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. For patients who suffer from bronchial asthma, the risk/benefit should be weighed before prescribing. To minimise systemic absorption of the active ingredient of these eye drops, pressure should be applied for one minute on the tear duct after application. Hands should be washed immediately after use of the drops to remove traces of the medication from the fingers. The drops should be discarded no later than 4 weeks after first opening the container.
Pregnancy:
There are no adequate and well-controlled studies in pregnant women. Pilopress 2% [Pilocarpine nitrate Ophthalmic Solution] should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation:
Pilocarpine nitrate has been detected in human milk following ophthalmic drug administration. Because of the potential for serious adverse reactions from Pilopress 2% [Pilocarpine nitrate Ophthalmic Solution] in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Pediatric Use: Appropriate studies on the effects of paediatric dosage have not been performed. However, no paediatric-specific problems have been documented to date.
Carcinogenicity, Mutagenicity:
No definitive long term animal studies have evaluated the carcinogenic potential of pilocarpine hydrochloride. |
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DRUG INTERACTIONS |
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. |
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Adverse Reaction |
* The most frequent adverse effects upon instillation of Pilopress 2% [Pilocarpine nitrate Ophthalmic Solution] are: temporary blurred vision, burning, stinging, redness or watering of the eyes, decrease in night vision, eye irritation, headache or browache.
* Less frequent to rare: eye pain
* Adverse reactions associated with systemic absorption include: increased sweating, muscle tremors, nausea, vomiting, diarrhoea, watering of the mouth, difficulty in breathing or wheezing. |
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Overdose |
Dilution with water and other fluids IS the usual response to accidental or deliberate overdose. |
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Presentation |
Carpinol 2% [Pilocarpine nitrate] is available in 5 ml bottle |
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