Flashcards in Cholinergic Drugs Deck (69):
List the direct acting cholinergic agonists
What drug is a cholinnesterase regenerator?
What muscarinic antagonist is used for motion sickness?
What muscarinic antagonists are used for GI disorders?
What anti muscarinic drugs are used in ophthalmology?
What antimuscarinic drugs are used for respiratory disorders such as asthma and COPD?
What antimuscarinic drugs are used for urinary disorders?
What antimuscarinic drugs are used for cholinergic poisoning?
Atropine + Pralidoxime
What antimuscarinic drugs are used or movement disorders?
What drugs are considered ganglion blockers?
Where are M1 receptors located and what signaling cascade do they utilize?
Where are M2 receptors located and what signaling cascade do they utilize?
Where are M3 receptors located and what signaling cascade do they utilize?
Where are M4 receptors located and what signaling cascade do they utilize?
Where are M5 receptors located and what signaling cascade do they utilize?
Where are Nm receptors located and what signaling cascade do they utilize?
Pentamer -> alpha2/betadelta; use Na/K depolarizing channel
Where are Nn receptors located and what signaling cascade do they utilize?
Postganglionic cell body
alpha and beta only; Na/K depolarizing channel
What cholinergic receptors are found on skeletal muscle?
Only nAChRs, so only those agents that activate nAChRs produce any effect (muscle contraction)
All cardiac actions of the PNS are mediated by what cholinergic receptor?
T/F: PNS innervation of the ventricles is much less extensive than that of the atria and activation of ventricular mAChRs cause much less physiologic effects than mAChR activation in the atria
In the GI and GU tracts, The ____ mAChR is required for direct activation of smooth muscle contraction
In the GI and GU tract, the ______ mAChR reduces cAMP formation and reduces relaxation caused by adrenergic effects (this results in contraction)
Sphincter relaxation in the GI and GU tract is via _____ signaling mediated by _____ mAChRs
The brain is relatively richer in __________ cholinergic receptors while the spinal cord contains predominately _________ cholinergic receptors
mAChhRs in brain and nAChRs in SC
What cholinergic drug is approved for intraocular use during surgery, causes miosis and is rarely given systemically?
What cholinergic drug is administered by inhalation for the diagnosis of Ron hill airway hyperactivity in pts who dont have clinically apparent asthma?
**Rarely used due to need for emergency resuscitation equipment
What selective mAChR agonist can be used to treat pts with urinary retention and heartburn and may produce a UTI if the sphincter fails to relax?
What drug is a nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or ophthalmic exam?
What cholinergic drug is an oral tablet used to treat dry mouth (xerostomia) in pts with Sjögren’s syndrome?
What drug is a pure mAChR agonist approved for xerostomia tx in pts with Sjögren’s syndrome or head and neck cancer treatment related xerostomia, miosis during ophthalmic procedures and glaucoma?
What is the most common adverse effect of Varenicline?
**Must stop immediately is behavioral changes are noticed
What is the most important use of AChEsterase inhibitors?
Tx of myasthenia gravis
Explain the MOA of Varenicline
- Partial agonist that binds with high affinity and selectivity to nAChR’s located in the brain to stimulate receptor-mediated activity but at a lower level than nicotine
- stimulation and subsequent sustained release of dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation
What are the 3 chemical groups of acetylcholinesterase inhibitors?
Carbamic acid esters
What are examples of AChEsterase inhibitors that contain an alcohol group and a quaternary ammonium group?
What is an example of an AChEsterase inhibitor that contains carbamic acid esters of alcohols bearing quaternary or tertiary ammonium groups
Psyostigmine, donepezil, tacrine, rivastigmine, and galantamine are all examples of what type of AChEsterase inhibitors?
Tertiary and uncharged
AChE inhibitors can reverse the paralysis induced y neuromuscular blocking drugs during surgical anesthesia. What 2 drugs are preferred for this?
What drug is used as an antidote to anti cholinergic intoxication?
Nondepolarizing neuromuscular blocking agents combined with AChE inhibitors will diminish the neuromuscular blockade. One exception is ____________ which is metabolized by plasma AChE causing the neuromuscular blockade to be prolonged
A combination of beta blockers and AChE inhibitors may enhance what symptom?
Coadministration of systemic corticosteroids with AChE inhibitors may affect what pts?
May enhance muscle weakness in pts with myasthenia gravis
What are the dominant initial signs of AChE intoxication?
Current antidotal therapy for organophosphate exposure resulting from warfare, terroism, or other sources of parenteral atropine are _____________ and a _______________ as an anticonvulsant
Atropine is a naturally occurring tertiary amine alkaloid ester found int he plant Atropa belladonna The tertiary amines are used for their effects on the eye or CNS system. There are 3 of these, what are they?
Atropine is a naturally occurring tertiary amine alkaloid ester found in the plan Atropa belladonna. The quaternary amines are charged and elicit their antimuscarinic effects in the periphery. There are 2 of these, what are they?
Parasympathetic effects of antimuscarinic compounds decline rapidly in all organs except ______________ where effects can last for 72 hours or longer
What tissues are most sensitive to atropine?
Salivary, bronchial and sweat glands
** acid secretion by the gastric parietal cells is the least sensitive
T/F: mAChR antagonists have no significant effect on the uterus
MAChR antagonists particularly the long-lasting _________________, are used to prevent synechia formation in uveitis and irititis
What is the first line therapy in the treatment of asthma and COPD?
What is the first drug of choice for symptomatic bradycardia in an advanced cardiac life support setting?
The prototype antimuscarinic agent used in disorders of the GU tract is ___________, which is somewhat selective for M3 mAChRs with side effects that include dry mouth, dizziness, constipation, blurred vision, dry eyes and UTI’s
____________ is a nonselective antimuscarinic agent that is comparable in efficacy and side effects with oxybutynin
_____________, _____________, and _____________ are antimuscarinic agents that are selective for the M3 subtype and are advantageous bc of their longer half-lives and reduced incidence of xerostomia and constipation
Darifenacin, solifenacin, tolterodine
What agents are utilized to treat both CNS and peripheral effects of excessive stimulation of mAChRs due to cholinergic poisoning?
Tertiary antimuscarinic agents, preferably atropine
___________agents are contraindicated in pts with glaucoma and should be used with cation inn elderly men with a history of BPH
Nonselective antimuscarinic agents (atropine) should be avoided in pts with _________ Disease, however, those that are selective may be of benefit
_____________ is selective for M1 and inhibits gastric secretion by acting at the ganglia
**Has little effect on SM or CNS and doesnt have the GI and CNS associated side effects that nonspecific mAChR antagonists have
All ganglion blocking drugs are synthetic ____________
________________ is a tertiary amine and was developed from initial ganglion blockers and has improved GI tract absorption
What is the MOA of ganglion-blocking drugs?
Ganglion-blocking drugs competitively lock the action of ACh and similar agonists at nAChRs of both parasympathetic and sympathetic autonomic ganglia
Where in the body is parasympathetic innervation absent?
What effects do ganglion blocking drugs have on the CNS?
Uncharged ones (mecamylamine) cross the BBB and cause sedation, tremor, choreiform movements, and mental aberrations
What effects do ganglion-blocking drugs have on the eye?
- cycloplegia wwith loss of accommodation
- moderate dilation of the pupil bc PNS tone usually dominates
What effects do ganglion blocking drugs have on the CV system?
- decreased BP
- diminished contractility and moderate tachycardia of the heart
What effect do ganglion-blocking drugs have on the GI tract?
Reduced secretion and profoundly inhibited motility
What effect do ganglion-blocking drugs have on the GU system?
- urination hesitancy and possible urinary rention in men with BPH
- erection and ejaculation may be prevented