What are the drugs classified as Anticholinergic (antimuscarinic)?

(13)

Atropine               Scopolamine

Dicyclomine          Propantheline

Glycopyrrolate      Ipratropium

Tiatropium           Benztropine

Trihexyphenidyl    Tolterodine

Oxybutynin          Solifenacin

Tropicamide

Atropine

(Hyoscyamine)

Anticholinergic drug

1.  naturally occuring belladonna alkaloid found in deadly nightshade
2. racemic mixture of d, l-hyoscyamine, where the "l" isomoer is more active

Describe Atropine's effects on...

Heart

Blood Vessels

Eye

GI Tract

Urinary Tract

Sweat Glands

Salivary Glands

Respiratory Tract

CNS

Heart-Tachycardia, increase cardiac output

Blood Vessels- reverse hypotensive actions of acetylcholine or other muscarinic agents. (Constrict)

Eye- three effects. a)mydriasis, pupil dialation.

b)cycloplegia, paralysis of accommodation

c)increases Intraocular pressure.

GI Tract- Inhibits motiliy and tone.  (antispasmodic action)

Urinary Tract- relaxes body, contracts sphincter (Ur. ret)

Sweat Glands- inhibit sweating and raises body temp.  (Children very sensitive to this.

Salivary Glands- inhibits the secretion of saliva.

Respiratory Tract- dries secretions. some bronchodialation.

CNS- LOW DOSE- sedation.  HIGH DOSE- stimulant. MODERATE-HIGH- hallucinogenic effects.

Scopolamine

(Hyoscine)

and 

Methscopolamine

Anticholinergic Drugs

Methscopolamine is quaternary analog that DOESN'T CROSS BLOOD-BRAIN BARRIER!!

Scopolamine is natural product found in plant Hyoscyamus niger

Anticholinergic effects, but more of a CNS sedation

Available in oral and patch form (Prevents vertigo and motion sickness)

Dicyclomine 

(bentyl)

Anticholinergic Drug

Nonquaternary Antimuscarinic agent

Intestinal antispasmatic for IBS

Propantheline

(pro Banthine)

Antimuscarinic agent

antispasmadic for IBS

Dries resp. Secretions

Few effects in CNS (quaternary, can't really pass BBB)

Ipratropium and Tiatropium

(Atrovent and Spiriva)

Glycopryyolate 

(robinul)

Benztropine and Trihexyphenidyl

(cogentin and Artane)

Tolterodine, Oxbutynin, Solifenacin

(Detrol, Ditropan, VESIcare)

Tropicamide

(Midriacyl)

Pancuronium (Pavulon)

Competetive Ach Antagonist (Nondepolarizing blocker)

act at the Neuromuscular junction and relax skeletal muscle.

Succinylcholine (Anectine)

Depolarizing agent, initially stimulates receptors to cause weak contractions, then relaxation and paralysis is seen

Therapeutic Effects of Anticholinergic Drugs

1. Treatment of GI Disorders (Cramps, IBS, Sweating)
2. Urology- treatment of urinary incontinence
3. Mydriatic agent (Dialation)
4. Cardiac Stimulation in emergence of Surgery
5. treatment of asthma and COPD (Bronchodialator)
6. Dries Respiratory Secretions

Pharmacologic Effects of Antimuscarinic Drugs

(to act as competetive antagonists at muscarinic receptors resulting in:)

1. Drying of secretions
2. Decrease tone and motility of GI
3. Relaxation of bladder and urine retention
4. Bronchodilation
5. mydriasis (dilation of pupil) and cycloplegia (loss of accomodation) and INCREASE in Intraocular Pressure
6. Increased Heart Rate (Atropine may initially cause sedation, then upon higher dose cause seizures)
7. CNS- Low dose-->sedation and amnesia High Dose--> exitation and seizure, toxic.  Quaternary salts don't cross blood brain barrier, no effect.

1. Glaucoma (already have high intraocular pressure)
2. Prostatic Hypertrophy
3. Cardiovascular Instability
4. Severe Ulcerative Colitis (colon could distend)