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TL anticholinergic
Cholinergic blocking drugs
| Question | Answer |
|---|---|
| How do cholinergic blocking or anticholinergic drugs work? | They interrupt the nerve impulses in the central and autonomic nervous system and prevent acetylcholine from stimulating cholinergic receptors. |
| Cholinergic blocking drugs don’t block all types of cholinergic receptor sites. Which ones do they block? | The receptor sites that are stimulated by the alkaloid muscarine or muscarinic receptor sites. |
| What is the prototype cholinergic blocking drug? | Atropine |
| Say Homatropine. | Home MAT tro peen |
| Say Hyoscyamine. | Hi uh SIGH uh mean |
| Say methscopolamine. | meth scope POLE uh mean |
| Say scopolamine. | Scope Paula mean |
| Name six belladonna alkaloids. | Atropine, belladonna, homatropine, hyoscyamine, methscopolamine, scopolamine |
| Name two synthetic derivatives of belladonna alkaloids (quaternary ammonium drugs). | Glycopyrrolate, propantheline |
| Name 5 tertiary amines (BDOTT). | benztropine, dicyclomine, oxybutynin, trihexyphenidyl, tolterodine |
| Which of the tertiary amines are used almost exclusively for Parkinson’s disease? | Benztropine and trihexyphenidyl |
| Name the one quaternary amine. | trospium |
| Which drug is used as an antidote to nerve agents? | Atropine |
| What routes are used to deliver anti-cholinergics? | Topical-eyes, PO – GI tract, mucous membranes, skin, and for quick action - IV |
| How do the later version anti-cholinergics compare to the belladonna alkaloids in GI absorption. | They are primarily absorbed through the GI tract but not as readily as belladonna alkaloids. |
| Discuss distribution in the body of belladonna alkaloids differs from the quaternary ammonium derivatives and dicyclomine. | Belladonna alkaloids are distributed more widely than quaternary ammonium derivatives and dycylomine. Belladonna alkaloids readily cross the BBB, the other drugs don’t. |
| Discuss metabolism and excretion of belladonna alkaloids. | Only slightly to moderately bound to protein leaving abundant drug available for therapeutic use in the body; metabolized in liver and excreted in urine |
| Discuss the metabolism and excretion of quaternary ammonium drugs. | hydrolyzed into simpler compounds in the GI tract and liver; excreted in feces and urine |
| Discuss the metabolism and excretion of dicyclomine. | metabolism unknown, but excreted in feces and urine |
| What’s weird about the pharmacodynamics of cholinergic blockers? | They have paradoxical effects on the body depending on the dose and condition being treated. They can stimulating or depressing effect depending on the target organ. |
| What’s weird about how cholinergic blockers work in the brain? | low drug levels stimulate and high drug levels depress |
| Use Parkinson’s disease as an example to explain how a condition can affect the effects of anti-cholinergic drugs. | Parkinson’s disease results from lack of dopamine to calm down effects of acetylcholine – so anti-cholinergics depress this effect, but in other disorders they stimulate the CNS. |
| Name some uses for anticholinergics related to the GI tract. | to treat spastic or hyperactive GI conditions; before endoscopy and sigmoidoscopy to relax GI smooth muscle |
| Why are quaternary drugs such as propantheline preferred for bladder and GI conditions? | less side effects |
| How are anticholinergics used for bladder conditions? | to relax the bladder and treat urinary incontinence |
| What drugs are used in conjunction with morphine to treat biliary colic? | belladonna alkaloids |
| How are anticholinergics used in surgery? | atropine to reduce oral, gastric and respiratory secretions; and to prevent drop in heart rate due to vagal stimulation during anesthesia; Scopolamine with morphine or meperidine for drowsiness and amnesia. |
| How are belladonna alkaloids use to treat the heart? | to treat symptomatic bradycardia ; to treat arrhythmias resulting from the use of anesthetics, choline esters, or succinycholine |
| How do belladonna alkaloids speed up the heart rate? | Impulses from the vagus nerve cause acetycholine activation of the SA and AV nodes resulting in slowed heart rate. Belladonna alkaloids compete with acetylcholine for receptor sites to preventing vagal stimulation. |
| What effects do cholinergic blockers have on the eye? | paralyze ciliary muscles, alter the shape of the lens, and dilate the pupils |
| Which two belladonna alkaloids are especially effective antidotes for cholinergic and anticholinesterase drugs and useful to counteract neuromuscular blocking drugs? | Atropine and hyoscyamine |
| Explain why cholinergic blocking drugs may increase the risk of toxicity of PO drugs. | Since cholinergic blocking drugs slow peristalsis and motility, drugs stay in the GI tract longer allowing for greater absorbtion and increased risk for toxicity |
| Name seven drug types that would increase the effects of cholinergic blocking drugs. | antiarrhythmics, antidyskinetics, antiemetics, antivertigos, antipsychotics, muscle relaxants, tricyclic and tetracyclic antidepressants |
| Name an antiarrhythmic that would increase the effects of a cholinergic blocking drug. | Norpace (disopyramide) |
| Give an example of an antidyskinetic that would increase the effects of an cholinergic blocking drug. | amantadine |
| Give three examples of antiemetics that would increase the effects of an anticholinergic drug. | buclizine, cyclizine, meclizine |
| Give an example of an antivertigo drug that could increase the effects of an anticholinergic drug. | diphenhydramine |
| Give 3 examples of antipsychotics that could interact with an anticholinergic drug and increase the effects. | haloperidol, phenothiazines, thioxanthenes |
| Name two muscle relaxants that could increase the effects of anticholinergic drugs. | cyclobenzaprine (Flexeril ); Orphenadrine – (Norflex) |
| Name two drug classes that would decrease the effectiveness of an anticholingergic drug. | cholinergic agonists like bethanechol; anticholinesterases like neostigmine and pyridostigmine |
| What happens when digoxin is taken with an anticholinergic? | increased risk for digoxin toxicity |
| What happens if an opiate analgesic and an anticholinergic are taken together? | further slowing of peristalsis |
| What interaction takes place between nitroglycerin and anticholinergics? | slowed absorption of nitroglycerin tablets placed under the tongue |
Created by:
Perseverandovercome
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