PRACTICAL APPLICATIONS OF THE AUTONOMIC DRUGS

CHOLINERGIC DRUGS

I. THEORETICAL PART

CLASSIFICATION

Parasympathomimetic drugs
 Direct acting (stimulating the nicotinic or muscarinic receptors)
o Choline esters: ACETYLCHOLINE, CARBACHOL, METHACOLINE,
BETHANECHOL
o Natural alkaloids: PILOCARPINE, ARECOLINE, MUSCARINE, NICOTINE
 Indirect acting
o Reversible cholinesterase inhibitors: NEOSTIGMINE, PHYSOSTIGMINE,
PYRIDOSTIGMINE, EDROPHONIUM, DONEPEZIL
o Irreversible cholinesterase inhibitors (organophosphate compounds):
ECHOTHIOPHATE, ISOFLUROPHATE, MALATHION

Cholinergic antagonists
 Natural: ATROPINE, SCOPOLAMINE
 Synthetic: PIRENZEPINE, HOMATROPINE, PROPANTELINE,
TRIHEXYPHENIDYL, TROPICAMIDE, BUTILSCOPOLAMINE

GENERAL PRINCIPLES OF ADMINISTRATION

1. Acetylcholine is used in eye surgery as ophtalmic solution instillation in the anterior

chamber to obtain miosis and prevent the anterior movement of the crystalline
implant.
2. Bethanechol stimulates the atonic urinary bladder or intestine after surgical
procedures, but with cholinergic adverse effects: sweating, hypersalivation, skin
congestion, low blood pressure, nausea, abdominal pain, diarrhea and
bronchoconstriction. To treat bradycardia or bronchoconstriction we can administer
Atropine sulphate.
3. Carbachol is indicated only in glaucoma. Miosis appears after 10-20 minutes and the
intraocular pressure decreases after 4-8 hours.
4. Pilocarpine is used in the emergency treatment of gaucoma. The latency is of a few
minutes. Pilocarpine intoxication is characterised by intense sweating and
hypersalivation, which is treated with parenteral Atropine.
5. Neostigmine and Physostigmine are administered in atonic urinary bladder or
intestine.
6. Atropine is indicated in preanestesia, bradycardia or atrioventricular block, as an
antispastic drug or antidote in intoxication with parasympathomimetics. Applied
locally, it produces cycloplegia and prolonged mydriasis (7 days). Side effects of
Atropine include: dry mouth, constipation, photophobia and urinary retention. The
intoxication include the following symtoms: mydriasis, photophobia, tachycardia,
dysphagia, constipation, urinary retention, hyperthermia, hallucinations and coma. The
best treatment is the administration of Physostigmine IV and benzodiazepines.
7. Atropine should not be administered in patients with glaucoma, prostate adenoma or
pyloric stenosis.
 8. Scopolamine is one of the most efficient treatments in motion sickness, useful in
preanestesia, Parkinson’s disease, billiary or renal colic.
9. Homatropine, Ciclopentolat and Tropicamide are indicated to obtain mydriasis, with a
shorter duration of action compared to Atropine.

Generic drug Brand name Route of Pharmaceutical

administration dosage form
Acetylcholine Miochol intraconjunctival opht. sol. 1%
Carbachol Isopto carbachol intraconjunctival opht. sol. 3%
Bethanechol Urecholine p.o. tab.5mg,10mg,
25mg, 50mg;
SC vial 50mg/10ml;
Pilocarpine Dropil intraconjunctival opht. sol. 2%, 1-2
drops, 3-4x/day
Isopto Carpine intraconjunctival opht. sol. 1%, 2%
Pilogel intraconjunctival opht. gel 4%
Ocusert pilo-20 intraconjunctival opht. insert
20μg/h; 40μg/h
Ocusert pilo-40 intraconjunctival
Neostigmine Miostin p.o.; tab. 15 mg,
SC, IV slow vial 0,5‰
Physostigmine Ezerina intraconjunctival eye drops 0,5%,
1% (4 - 6 x 1
drops/day)
Atropine sulphate Atropina SC, IM, IV vial 0,25‰; 1‰;
slow; eye drops 1%
intraconjunctival
Scopolamine Scopoderm TTS retroauricular 0,5mg/72h;
1mg/72h
Butylscopolamine Scobutil p.o. tab.10mg;
IM vial 10mg/1ml
Propanteline Propantelina p.o. dg. 15mg
Pirenzepine Gastrozepin p.o. tab. 25 mg
Homatropine Homatropina intraconjunctival eye drops 1%
Ciclopentolat Ciclopentolat intraconjunctival eye drops 1%
Tropicamide Mydrum intraconjunctival opht. sol. 0,5%

II. PRACTICAL PART

1. Write a medical prescription to a patient with chronic glaucoma.
2. Write a medical prescription to a patient with myasthenia gravis.
3. Write a medical prescription to a patient with renal colic.
4. Prescription: Atropine sulphate 0,5mg IV bolus.
Avialable: Atropine sulphate 1‰, vial 1ml.
Calculate how many ml to administer.