Atropinol - General Information
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly solanaceae.
Pharmacology of Atropinol
Atropinol, a naturally occurring belladonna alkaloid, is a racemic mixture of equal parts of d- and l-hyoscyamine, whose activity is due almost entirely to the levo isomer of the drug. Atropinol is commonly classified as an anticholinergic or antiparasympathetic (parasympatholytic) drug. More precisely, however, it is termed an antimuscarinic agent since it antagonizes the muscarine-like actions of acetylcholine and other choline esters. Adequate doses of atropine abolish various types of reflex vagal cardiac slowing or asystole. The drug also prevents or abolishes bradycardia or asystole produced by injection of choline esters, anticholinesterase agents or other parasympathomimetic drugs, and cardiac arrest produced by stimulation of the vagus. Atropinol may also lessen the degree of partial heart block when vagal activity is an etiologic factor. Atropinol in clinical doses counteracts the peripheral dilatation and abrupt decrease in blood pressure produced by choline esters. However, when given by itself, atropine does not exert a striking or uniform effect on blood vessels or blood pressure.
Atropinol for patients
When atropine and pralidoxime are used together, the signs of atropinization (flushing, mydriasis, tachycardia, dryness of the mouth and nose) may occur earlier than might be expected than when atropine is used alone because pralidoxime may potentiate the effect of atropine.
The following precautions should be kept in mind in the treatment of anticholinesterase poisoning although they do not bear directly on the use of atropine and pralidoxime. Since barbiturates are potentiated by the anticholinesterases, they should be used cautiously in the treatment of convulsions.
In the face of life-threatening poisoning by organophosphorous nerve agents and insecticides, there are no absolute contraindications for the use of atropine.
Additional information about Atropinol
Atropinol Indication: For the treatment of poisoning by susceptible organophosphorous nerve agents having cholinesterase activity as well as organophosphorous or carbamate insecticides.
Mechanism Of Action: Generally, atropine lowers the "rest and digest" activity of all muscles and glands regulated by the parasympathetic nervous system. This occurs because atropine is a competitive inhibitor of the muscarinic acetylcholine receptors (acetylcholine is the neurotransmitter used by the parasympathetic nervous system).
Drug Interactions: Not Available
Food Interactions: Avoid alcohol.
Take with food.
Generic Name: Atropine
Synonyms: Atropin [German]; Atropina [Italian]; Atropine Sulfate; DL-Hyoscyamine; DL-Tropyl tropate
Drug Category: Adjuvants, Anesthesia; Anti-Arrhythmia Agents; Bronchodilator Agents; Muscarinic Antagonists; Mydriatics; Parasympatholytics
Drug Type: Small Molecule; Approved
Other Brand Names containing Atropine: Atnaa; Atropair; Atropen; Atropin; Atropin-flexiolen; Atropine Care; Atropine Sulfate Ansyr Plastic Syringe; Atropine Sulfate S.O.P.; Atropinol; Atropisol; Atrosulf; Equipin; Eyesules; Homapin-10; Homapin-5; I-Tropine; Isopto Atropine; Isopto-atropine; Minims Atropine; Ocu-Tropine; Tropine tropate; Troyl tropate;
Absorption: Atropine is rapidly and well absorbed after intramuscular administration. Atropine disappears rapidly from the blood and is distributed throughout the various body tissues and fluids.
Toxicity (Overdose): Oral, mouse: LD50 = 75 mg/kg. Symptoms of overdose includes widespread paralysis of parasympathetically innervated organs. Dry mucous membranes, widely dilated and nonresponsive pupils, tachycardia, fever and cutaneous flush are especially prominent, as are mental and neurological symptoms. In instances of severe intoxication, respiratory depression, coma, circulatory collapse and death may occur.
Protein Binding: The protein binding of atropine is 14 to 22% in plasma.
Biotransformation: Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver. From 13 to 50% is excreted unchanged in the urine.
Half Life: 3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter (approximately 20 minutes) in females than males.
Dosage Forms of Atropinol: Solution Intravenous
Solution / drops Oral
Chemical IUPAC Name: [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate
Chemical Formula: C17H23NO3
Atropine on Wikipedia: http://en.wikipedia.org/wiki/Atropine
Organisms Affected: Humans and other mammals