Pilocarpine

Pilocarpine Brand Names

Adsorbocarpine | Akarpine | Isopto Carpine | Ocu-Carpine | Pilocar | Pilopine HS | Salagen

What is Pilocarpine

Pilocarpine is an alkaloid derived from the leaflets of Pilocarpus microphyllus or jaborandi. The alkaloid was isolated in 1875, and its muscarinic activity was described shortly thereafter.

Pilocarpine is particularly active on the sweat glands and eyes and is used to treat glaucoma. Pilocarpine also is used for miosis induction, both postoperatively and after ophthalmoscopic examination.

Ocular ‘systems’ are available, which are contact lens-type devices that provide a 7-day treatment. Ophthalmic solutions are preferred over the device when an intense miotic response is indicated.

The FDA approved the ophthalmic solution in 1974. An ocular system that releases pilocarpine continuously, Ocusert, was approved by the FDA in 1974. In 1994, an oral formulation for the treatment of symptoms of xerostomia caused by radiotherapy for cancer of the head and neck was approved by the FDA.

Pilocarpine tablets (Salagen) were approved February 1998 for the management of symptoms associated with Sjogren’s syndrome.

Indications

1. glaucoma
2. increased intraocular pressure
3. miosis induction
4. ocular hypertension
5. xerophthalmia
6. xerostomia

For the treatment of increased intraocular pressure (IOP) in patients with glaucoma or ocular hypertension or for the prevention of increased IOP associated with laser surgery

Side Effects

1. abdominal pain
2. alopecia
3. amblyopia
4. angina
5. anorexia
6. anxiety
7. aphasia
8. appetite stimulation
9. arthralgia
10. asthenia
11. blurred vision
12. bone fractures
13. bradycardia
14. chest pain (unspecified)
15. chills
16. cholelithiasis
17. ciliary body spasm
18. colitis
19. confusion
20. conjunctivitis
21. contact dermatitis
22. depression
23. diarrhea
24. dizziness
25. drug-induced body odor
26. dyspepsia
27. dysphagia
28. dyspnea
29. dysuria
30. edema
31. emotional lability
32. epistaxis
33. eructation
34. erythema nodosum
35. esophagitis
36. exfoliative dermatitis
37. flushing
38. gastritis
39. gingivitis
40. headache
41. hematuria
42. hepatitis
43. hiccups
44. hyperhidrosis
45. hyperkinesis
46. hypertension
47. hypoglycemia
48. hypotension
49. hypothermia
50. increased urinary frequency
51. insomnia
52. lacrimation
53. laryngitis
54. laryngospasm
55. leukopenia
56. lymphadenopathy
57. melena
58. menorrhagia
59. migraine
60. miosis
61. myasthenia
62. myocardial infarction
63. myopia
64. nausea
65. night blindness
66. ocular irritation
67. ocular pain
68. palpitations
69. pancreatitis
70. paresthesias
71. peripheral edema
72. photophobia
73. pruritus
74. pyuria
75. rash
76. retinal detachment
77. seborrhea
78. sinus tachycardia
79. skin ulcer
80. syncope
81. thrombocytopenia
82. thrombosis
83. tremor
84. urinary urgency
85. vaginal pain
86. visual impairment
87. vomiting
88. xerosis
89. xerostomia
90. yawning

Monitoring Parameters

• intraocular pressure
• ophthalmologic exam

Contraindications

• asthma
• biliary tract disease
• breast-feeding
• bronchitis
• cardiac disease
• children
• cholelithiasis
• chronic obstructive pulmonary disease (COPD)
• closed-angle glaucoma
• contact lenses
• driving or operating machinery
• hepatic disease
• infants
• iritis
• neonates
• nephrolithiasis
• pregnancy
• psychosis
• retinal detachment
• sulfite hypersensitivity
• uveitis

Interactions

• Acebutolol
• Ambenonium Chloride
• Amoxapine
• Anticholinergics
• Atenolol
• Atenolol; Chlorthalidone
• Atropine
• Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
• Atropine; Difenoxin
• Atropine; Diphenoxylate
• Atropine; Edrophonium
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Belladonna; Opium
• Bendroflumethiazide; Nadolol
• Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
• Benztropine
• Beta-blockers
• Betaxolol
• Bethanechol
• Bisoprolol
• Bisoprolol; Hydrochlorothiazide, HCTZ
• Brimonidine; Timolol
• Carteolol
• Carvedilol
• Cevimeline
• Chlordiazepoxide; Clidinium
• Chlorpromazine
• Cholinesterase inhibitors
• Codeine; Phenylephrine; Promethazine
• Codeine; Promethazine
• Dextromethorphan; Promethazine
• Dicyclomine
• Disopyramide
• Donepezil
• Donepezil; Memantine
• Dorzolamide; Timolol
• Edrophonium
• Esmolol
• Flavoxate
• Fluphenazine
• Galantamine
• Glycopyrrolate
• Glycopyrrolate; Formoterol
• Guanidine
• Homatropine; Hydrocodone
• Hydrochlorothiazide, HCTZ; Metoprolol
• Hydrochlorothiazide, HCTZ; Propranolol
• Hyoscyamine
• Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
• Indacaterol; Glycopyrrolate
• Labetalol
• Levobetaxolol
• Levobunolol
• Maprotiline
• Mepenzolate
• Meperidine; Promethazine
• Mesoridazine
• Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
• Methscopolamine
• Metoprolol
• Nadolol
• Nebivolol
• Nebivolol; Valsartan
• Neostigmine
• Oxybutynin
• Penbutolol
• Perphenazine
• Perphenazine; Amitriptyline
• Phenothiazines
• Phenylephrine; Promethazine
• Physostigmine
• Pindolol
• Pralidoxime
• Prochlorperazine
• Promethazine
• Propantheline
• Propranolol
• Pyridostigmine
• Rivastigmine
• Scopolamine
• Sotalol
• Tacrine
• Thiethylperazine
• Thioridazine
• Timolol
• Tricyclic antidepressants
• Trifluoperazine
• Trihexyphenidyl
• Trospium