All the Drug structure + facts that might be k types in cholinergic lec 6-8

Cevimeline

Quinuclidine analog and a mAChR M3 agonist

available as oral capsule for treatment of dry mouth associated with Sjogren syndrome

side effects include nausea, vomiting diarrhea, excessuve sweating, blurred vision, and difficulty sleeping

What is this

Pilocarpine

Musacrinic agonist primarily acts on M3 mAChR

Natural alkaloid with a pKa of 6.8

naturally occuring alkaloid is 3S,4R (+)

used for treatment of symptoms of sjogren syndrome (an immune disorder which destroys glands, resulting in dry eyes and dry mouth)

Pilocarpine can stimulate the secretion of tearsa and saliva

Prone to hydrolysis and epimerization, and the gel forumlation needs to be refridgerated and labeled with a 2-week expiration date

What is this

Bethanechol

selecetive agonist for mAChRs

not hydrolyzed by AChE and have long duration of action

given ORALLY for the treatment of ileus and urinary retention

What is this

Carbachol

a carbamate analog of acetylcholine

more resistant towards acid-, base- or AChE-catalyzed hydrolysis than acetylcholine

agonist of both mAChRs and nAChRs (non-selective)

used in the treatment of glaucoma and for the induction of miosis in ocular surgery

What is this

methacholine

Marketed as an enantiomeric mixture

SELECTIVE MUSCARINIC AGONIST and has LITTLE activity at nAChRs

S-enantiomer is 240-fold more potent than the R-enantiomer at mAChRs

S-enantiomer is more resistant to AChE hydrolysis than acetylcholine (54%), while R-enantiomer is a weak inhibitor

Methacholine is formulated for inhalation and used for the DIGNOSIS OF ASTHMA

what is this

Oxotremorine

used to treat Alzheimer's disease

selective for mAChRs in the brain

what is this

arecoline

used to treat Alzheimer's disease

selective for mAChRs in the brain

what is this

xanomeline

used to treat Alzheimer's disease

selective for mAChRs in the brain

what is this

nicotine

dibasic containign a weak basic pyridine nitrogen with a pka of 3.1 and a pyrrolidine nitrogen with a pKa of 8.0

dependence is attributed to its binding of the a4B2 nicotinic receptor subtype

what is this

buproprion

initially approved for the treatment of depression

formulated as a 12-hour sustained-release tablet under the tradename Zyban

first-line agent for smoking cessation

MOA unclear: likely involed several mechanisms including dopamine reuptake inhibition and norepinephrine reuptake inhibition

non-competitively blocks the activation of neuronal nAChRs by nicotine (nAChR ANTAGONIST)

what is this

Varenicline

a partial agonist at a4B2 and a full agonist at a7 nAChRs

used as an aid to smoking cession treatment

developed from structural studies of the substructures of both morphine and cyticine

what is this

edrophonium

(NOTE QUATENARY AMINE)

indirect cholinomimetic (AChE inhibitor)

used for the DIAGNOSIS of myasthenia gravis

shortest acting

what is this

Pyridostigmine

(NOTE QUATENARY AMINE)

indirect cholinomimetic (AChE inhibitor)

used for the TREATMENT of myasthenia gravis

longest acting

what is this

Neostigmine

(NOTE QUATENARY AMINE)

indirect cholinomimetic (AChE inhibitor)

used to reverse anesthesia post operation

treatment of myasthenia gravis

prolong the action of acetylcholine specifically at the neuromuscular junction

what is this

Donepezil

cholinesterase inhibitor

(NOTE THE TERTIARY AMINE)

used for the treatment of Alzheimer's

improve symptoms but do not prolong survival

what is this

Rivastigmine

cholinesterase inhibitor

(NOTE THE TERTIARY AMINE)

used for the treatment of Alzheimer's

improve symptoms but do not prolong survival

what is this

Galantamine

cholinesterase inhibitor

(NOTE THE TERTIARY AMINE)

used for the treatment of Alzheimer's

improve symptoms but do not prolong survival

what is this

Tacrine

cholinesterase inhibitor

(NOTE THE TERTIARY AMINE)

approved for the treatment of Alzheimer's but its use is limited due to hepatotoxicity

improve symptoms but do not prolong survival

what is this

Physostigmine

a reversible cholinesterase inhibitor used to treat glaucoma and anticholinergic toxicity (ANTIDOTE OF ATROPINE)

what is this

Pralidoxime

a strong nucleophile that competes with AChE for the phosphorus group of the inhibitor (organophosphate) and the enzyme (AChE) is restored

used as an antidote to treat organophosphate poisoning

must be given within 24-36 hours of poisoning otherwise the enzyme becomes reistant to the antidotal effects because of aging

what is this

Parathion

acts on the enzyme AChE indirectly

an oxidase replaces the double bonded sulfur with oxygen to give PARAOXON

applied by spraying as an insecticide, often applied to cotton, rice and fruit trees

what is this

atropine

muscarinic antagonist

used for the treatment of bradycardia and as a preoperative agent to reduce secretions before surgery

ANTIDOTE FOR ANTICHOLINESTERASES (organophosphate nerve agents and insecticides) and muscarine

what is this

Scopalamine

muscarinic antagonist

most used for the treatment of motion sickness

available in transdermal patch (behind the ear) and oral pills to prevent nausea and vomiting

what is this

Methylscopolamine

muscarinic antagonist

used for the treatment of pepic ulcer by reducing stomach acid secretion (oral)

binds to M1-M5 isoforms of muscarinic receptors

what is this

Diphenhydramine

first-generation histamine H1-receptor antagonist

used to prevent and treat nausea, vomitting and dizziness caused by motion sickness

also used to relieve symptoms of allergy, hay fever and the common cold

what is this

8-chlorotheophyline

and known as 1,3-dimethyl-8-chloroxanthine

stimulant drug of the xanthine chemical class with physiological effects similar to caffeine

stimulant help reduce drowsiness from benedryl

what is this

Oxybutin

muscarinic antagonist

decreases urinary urgency and frequency

marketed as racemic mixture, and the R-isomer is responsible for its anti-muscarinic action

what is this

Darifenacin

is an M3-selective anti-muscarinic that acts quickly to improve overactive bladder symptoms

what is this

Solifenacin

aminoalkyl ester

a highly selective M3 muscarinic antagonist used for the treatment of overactive bladder with less side effects

what is this

Trospium

the only quaternary anti-muscarinic available for overactive bladder

extended-release doasge form has an elimination half-life of 35 hours

what is this

Ipratropium

Short-acting muscarinic antagonist

poorly absorbed from the lungs and the quaternary ammonium prevents it from crossing the blood brian barrier and producing undesired side effects (inhaler or nebulizer)

15 mins onset of action and a short duration of action ( < 4 hours)

used to produce broncodilation in COPD

also used as nasal spray to treat rhinorrhea

what is this

Aclidinium bromide

Long acting muscarinic antagonist (broncodilator > 24 hours)

approved for inhalation treatment of COPD

quick onset

what is this

Umeclidinium

selective M3 muscarinic receptor antagonist

used as a dry powder inhaler and used together with vilanterol ( LABA ) in two different formulations for the treatment of COPD (INHALATION)

what is this

Tiotropium Bromide

Mainly acts of M3 muscarinic receptors as an antagonist

used for the relief of broncospasms associated with COPD

30 mins onset and a long duration of action ( > 24 hours) INHALATION

Administered by oral inhalation of an aerosol solution or a dry powder inhaler DO NOT TAKE ORALLY

what is this

Glycopyrrolate

LAMA

aminoalcohol ester

used for the treatment of COPD (inhalation)

also used to treat peptic ulcers, reduce excessive sweating

what is this

Revefenacin

LAMA ( >24 hours) for the treatment of COPD (inhalation)

similar affinity to the subtypes of muscarinic receptors M1 to M5

in the airways, it exhbits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to broncodilation

what is this

Clidinium

muscarinic antagonist

used in combination with chlordiazepoxide to treat peptic ulcers, IBS, constipation, and diarrhea), and enterocolitis. ORAL

what is this

Benzatropine

selective M1 muscarinic ACh receptor antagonist

oral drug to treat symptoms of Parkinsons diseases

what is this