Anticholinesterase

pharmacology is the most important part of the pharmacy field and every pharmacist should have the good knowledge about that and there are different parts and one important part is consists of the anticholinesterase drugs.

1. Anticholinesterase drugs By : Mehrasa Nikandish Subject : Pharmacology University of Georgia 2020-2021

2. Overview Introduction Receptors Classification Mechanism of action Therapeutic uses Adverse drug reactions

3. Introduction Cholinesterase inhibitors, also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter  acetylcholine or   butyrylcholine . This increases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others .

4. Receptors

5. Natural Alkaloids Atropine Hyoscine (Scopolamine) Semisynthetic derivatives Atropine methonitrate Homatropine Hyoscine butyl bromide Ipratropium bromide Tiotropium bromide Synthetic compounds Antisecretory - antispasmodics : 1. quaternary comps. : propantheline - oxyphenonium - clidinium - isopropamide 2. tertiary amines: diclycomine - valethamate - pirenzepine . Mydriatics : Cyclopentolate - Tropicamide Vasicoselective : oxybutynin – flavoxate - tolterodine . Antiparkinsonian : trihexyphenidyl ( benzhexol )- procyclidine - biperiden Classification

6. Mechanism of action Enzyme inhibition: inhibit the enzyme acetylcholinesterase reversibly- results in greater availability of ACH at its sites of action. Presynaptic effects: in the absence of nondepolarizing neuromuscular-blocking drugs, administration of an anticholinesterase drug may produce spontaneous contractions of skeletal muscles. Direct effects on the neuromuscular junction

7. Therapeutic uses

8. Therapeutic uses

9. Adverse drug reactions Nausea, increased salivation, increased sweating Flushing, Bradycardia Bronchospasm Abdominal pain, Diarrhea Increased urination At high doses: convulsions; skeletal muscle weakness ADR on eyes when used as eye drops: Miosis , decrease vision in Dim-light, Impaired accommodation.

10. Termination of further exposure to the poison fresh air, wash the skin and mucous memberanes with soap and water, gastric lavage according to the needs. Specific antidots : a) atropine b) cholinesterase reactivators Supportive measures: maintain blood pressure, hydration, control of convulsions with judicious use of diazepam. Maintain patent airway, positive pressure respiration if it is falling. Organophosphorous poisoning (treatment)

11. Organophosphorous poisoning (treatment)

12. Question time What are anticholinesterase drugs used for? Major contraindications to the use of muscarinic agonists  A) postoperative abdominal distention  B) asthma  C) treatment of diminished salvation, secondary to radiation  D) peptic ulcer  E) hyperthyroidism Answer: Reversal of nondepolarizers Answer: B-D-E

13. Thanks for your attention