Miotics - direct acting include- Acetyl choline, Carbachol, Pilocarpine Refer - Acetylcholine

 Mitotic and other occular hypotensive effect antagonised bylong term, topical/systemic cortico-steroids, systemic anticholinergics, antihistamines, meperdine hydrochloride, tricyclic antidepressants and sympathomimetics.

Concomittant admin of two miotics may make both drugs unresponsive and increased risk of allergic and toxic reaction. (The miotic and occular hypotensive effect of topical anticholinesterases inhibited).

Drug /Food interaction- The rate of absorption of pilocarpine is decreased when taken with a high fat meal. Maximum concentration is decreased and time to reach maximum concentration is increased

Lowering IOP

 Miotics - direct acting include- Acetyl choline, Carbachol, Pilocarpine Refer - Acetylcholine 

Body a whole- body odour, hypothermia, mucous membrane abnormality,

Cardiovascular- bradycardia, ECG abnormality, palpitations,syncope

GI- anorexia, increased appetite, esophagitis, GI disorder, tongue disorder Hematologic- leukopenia, lymphadenopathy

CNS- anxiety, confusion, depression, abnormal dreams, hyperkinesia, hypesthesia, nervousness, paresthesisas, speech disorder, twitching.

Respiratory- increased sputum, stridor, yawning

Special senses- deafness, eye pain, glaucoma

GU- dysuria, metrorrhagia, urinary impairment

Miscellaneous- seborrhea, - In two patients with underlying cardiovascular disease, one experienced a myocardial infarction and the other an episode of syncope.

Uncontroolle asthma, hypersensitivity to pilocarpine, when miosis is undesirable (eg. inacute iritis and in narrow -angle (angle closure) glaucoma.

Special precautions:

Toxicity- pilocarpine toxicity ischaracterized by an exaggeration of its parasympathomimetics effects. These may include- headache, visual disturbances, lacremation, sweating, respiratory distress,

GI spasm, nausea, vomiting,diarrhea, AV block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia tremors.

Biliary tract- administer with caution to patients with known or suspected cholelithiasis or biliary tract disease. Contractions of gallbladder or biliary smooth muscle could precipitate complications uncluding cholecystisis ,cholangitis and biliary obstruction.

Renal colic- pilocarpine may increase uretral smooth muscle tone and could theoretically precipitate renal colic ( or uretral reflux) particularly in patients with nephrolithiasis. Psychiatric disorders- cholinergic agonists may have dose related

CNS effects. Consider this when treating patients with underlying cognitive or psychiatric disturbances.

Warnings-

Cardiovascular disease- patients with signifiacant cardiovascular disease maay be unable to compensate for transcient changes in hemodynamics or rhythm induced by piolcarpine . Pulmonary edema has been reported as a complication of pilocarpine toxicity from high ocular doses given for acute angle-closure glaucoma. Administer pilocarpine with caution and under medical supervision in patients with cardiovascular disease.

The dose related cardiovascular effects of pilocarpine include hypotension, hypertension,bardycardia, and tachycardia.

Ocular effects- carefully examine the fundus prior to initiating therapy with pilocarpine. An association of occular pilocarpine use and retinal detachment in patients with preexisting retinal disease has been reported. The systemic blood level that is associated with this finding is not known

. Ocular formulations of pilocarpine have caused visual burning which may result in decreased visual acuity, especially at night and in patients with central lens changes and inpairment of depth perception

. Advice caution while driving at night or performing hazardous tasks in reduced lighting. Pulmonary disease- pilocarpine has been treported to increase airway resistence, bronchial smooth muscle tone and bronchial secretions

.Administer with caution and medical supervision in patients with controlled asthma, chronic bronchitis or chronic obstructive pulmonary disease.

Fertility- The possibility that pilocarpine may impair male fertitlity in humans cannot be rulred out.

Elderly- adverse reports by those > 65 and those < 65 yeras of age were comparable Of the 15 elderly volunteeers ( 5 women , 10 men ) the 5 women had a higher Cmax and AUC than the men.

Pregnancy- use during pregnancy only if the potential benefit justifies the potentail risk to the fetus.

Lactation- Because of the potential for serious adverse reactions in nursing infants decide whether to discontinue nursing or discontinue the drug depending upon the importance of the drug to the mother.

Children- safety and efficacy in children have not been established.

Indications:

Lowering IOP

Dosage:

Instil 1 or 2 drops into the eyes(2% soln)

1. Inform patients that pilocarpine may cause visual disturbances especially at night, that could impair their ability to drive safely

. 2. If a patient sweats excessively while taking pilocarpine and cannot drink enough liquid, the patient should consult a physician. Dehydration may develop.

3.Allergies- tell your doctor if you have ever had any unusual or allergic reaction to pilocarpine. Also tell your doctor if you are allergic to any other substances, such as foods, presevatives or dyes.

4.Pregnancy - Studies on effects of pregnancy have not been done. Before using this medicine make sure your doctor knows if you are prregnant or if you may become pregnant

5.Breast feeding- not known whether pilolcarpine passes into thebreast milk. No reported to cause problems to nursing babies.

6. Children - no specific information available comparing use in children with use in adults.

7.Elderly- not studied in older people. Not expected to cause any different problems than in younger adults.

8. Other medicines - Amantadine or Anticholinergics or Antidepressants or Antidykinetics for Parkinsons disesase or Antihistamines or Antipsychotics or Buclizine or Carbamazepine or Cyclizine or Cyclobenzaprine or Disopyramide or Flavoxate or Ipratropium or Meclizine or Methylphenidate or Orphendrine or Oxybutynin or Procainamide or Promethazine or Quinidine or Trimeprazine - pilocarpine may reduce the effect of these medicines or these medicines may reduce the effects of pilocarpine Antimyasthenics or Beta-blockers or Ophthalmic beta-blockers - pilocarpine may increase the side efects of these medicines Carbachol or Demecarium or Echothiophate or Isoflurophosphate or Physiostigmine or Pilocarpine - pilocarpine may increase the efects of these ophthalmic glucoma medicines

9. Other medical problems - Tell your doctor if you have any other medical problems especially - Asthma or Gallbladder problems or Glaucoma ,angle closure or Heart or blood vessel disease or Iritis or Kidney problems or Mental problems -pilocarpine may make the condition worse Retinal detachment or Retinal disease - pilocarpine may increase the risk of a detached retina

10. Missed dose - If you miss a dose of this medicine, take it as soon as possible. however, if it is almost time for the next dose, skip the missed dose. Do not double doses

. 11. Storage - Keep out of reach of children. Store away from heat or direct sunlight. Do not store the capsule in bathroom, near the kitchen sink, or in other damp places.

12. Outdated medicines - Do not keep outdated medicine or medicine no longer needed. Be sure that any discarded medicine is out of reach of children.

Pharmacology-

Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad septrum of pharmacologic effects with predominant muscrainic action.Pilocarpine in appropriate dosage can increase secretion by the exocrine glands.

The rate of absorption of pilopcarpine isdecraesed when taken with a high fat meal. Maximum concentration is decreased and time to reach maximum concentration is increased

Pregnancy-

Use during pregnancy only if the potential benefit justifies the potentail risk to the fetus.

Lactation-

Because of the potential for serious adverse reactions in nursing infants decide whether to discontinue nursing or discontinue the drug depending upon the importance of the drug to the mother.

Children-

Safety and efficacy in children have not been established.