Cholinergics Flashcards
M1
Nerves Gq
M2
Heart nerves smooth muscle
Gi
M3
Glands SM, endothelium
G1
M4
CNS Gi
M5
CNA Gq
Nm
Skeletal muscle
Pentameric a2bdelta game/epsilon
NaK depolarizing channel
Non
Postganglionic cells body , dendrites, CNS
A and b only
Na K depolarizing ion channel
Entropic
Misalignment of the eyes caused by hypermetropic accommodative error
Eye
M2, M3
Heart SA/AV
M2
Atria
M2
Ventricle
M2
Endothelium
M3
Glands
M2,3
Lung
M2,M3
Lung
M2,M3
GI
M2,M3
CNS
M1-M5
Most organs
M3 predominant
Heart
M2
Smooth muscle
M2,3
What direct agonists are susceptible to acetylcholinesterase
Methacholine a bit not carb or beth
Which direct cholinergic agonist has nicotonic cation
Carabachol
Muscadine
Charged but can cross the BBB and is highly toxic (muschrooms)
AChe inhibitors
Alcohols (reversible)
Carbamic acid esters-reversible but no longer lasting than alcohols
Organophosphate -irreversible (covalent)
Charged AChE inhibitor
Insoluble in lipids
Do not cross BBB, poor PO absorption
Edrophonium, pyridostigmine, neostigmine, echothiophate, ambenonium
Neutral AChe inhibitors
Can cross BBB and readily absorbed
Organophosphates
Tertiary agents (physostigmine, donepezil, galantamine, rivastigmine, tacrine)
Cevimeline
Direct acting cholinergic Oral tablet used to treat dry mouth in patients with sjorgen
Varenicline
Smoking cessation
Partial agonist bindsa4b2 Nn
Stimulation and sustained release of mesolimbic dopamineare thought to reduce craving and withdrawal symptoms
Adverse effects varenicline
Nausea, neuropsychiatric (behavior changes, agitation, depressed, suicidal, suicide)
Uses for direct acting cholinergic
Post op ileus, congenital megacolon, urinary retention, esophageal reflux, zerosterma, sjorgen
Who are muscarinic stimulants contraindicated in
Asthma, hyperthyroidism, coronary insuffiency, acid peptic disease
How get nicotine poisoning
Cigarettes and insecticides
Symptoms of nicotonic poisoning
CNS stimulation, skeletal muscle and end plat depolarization, respiratoy paralysis, hypertension, cardiac arrhythmia
How treat ACH toxicity
Atropine and an anticonvulsant(diazepam a anticonvulsant)
Drugs used for ophthalmology
Atropine, cyclopentolate, homatropine, scopolamine, tropicamide
Drugs for respirator
Tiotropium
Urinary drugs
Darifenacin Oxybutaynin Solifenacin Tolterodine Trospium
Drugs for movement disorders
Benztropine Biperiden Orphenadrine Procylidine Trihexyphenidyl
What are homatropine and atropine used for
Prevent synechia formation in uveitisand iritis -long acting mydriasis and cycloplegia for 14 days
Ipratopium and tiotropium
Tiotropium is longer
Bladder receptor to prevent urgency for anticholinergic
M3
What selective M3 drugs for preventing urinary urgency
Darifenacin, solifenacin, tolterodine
Longer half lives and reduced xerosterma and constipation
Contraindications for anticholinergics
Glaucoma
Prostatic hyperplasia
Acid peptic disease
Dopamine agonist
Fenoldpam D1 receptor
Dopamine equal D1=D2
Partial B agonists
Acebutolol
Labetalol
Pindolol
Penbutolol
Penbutolol
B1 and B2 non selective blocker
Partial b agonist and ISA
Block sympathetic effects but have submaximal effects
Less risk for bradycardia, increases VLDL/HDL and other effects of beta receptor blockade
Adverse effects of beta blockers
Sedation, sleep disturbances, depression
Increase VLDL and decrease HDL with chronic use
May exacerbate hypoglycemia in type 1 diabetes patients on insulin
Cocaine
Indirect adrenomimetics
Inhibits re uptake of DA and NE
Selegiline and phenelzine
Indirect adrenomimetics
Inhibitors of MAO
Amphetamines, methylphenidate, tyramine
Indirect adrenomimetics
Reverse NA and DA uptake mechanism and increase their release
Silicosis
A1 selective
Emphetamine and methamphetamine
Marked stimulant effect on mood and alertness
Decrease appetite
Drug abuse
Methylphenidate
Used in children with ADHD similar to amphetamine but has an abuse potential
Cocain
Inhibitors transmitter reuptake at adrenergic synapses
Peripheral and intense central action
Local anesthetic properties
Heavily abused
Phenelzine and selegiline
Inhibitors of MAO
Increase NE stores in CNA
Antidepressant action
Tyramine
Indirect adrenergic agonist
Product of tyrosine metabolism that is found in cheese, meats, smoked and pickled fish
Releases stored NE from presynaptic adrenergic terminals
Metabolized by MAO in liver
May lead to increase in BP in patients taking MOA inhibitors
Metytosine
Indirect acting inhibits synthesis of tyrosine hydroxilare at pre synaptic neuron
Guanethidine
Indirect acting prevents storage and depletes NE at synapse
Direct acting
Right on post synaptic neuron
Cocain
Indirect acts at synapse preventing reuptake
Phenelzine
MOA inhibitor in presynaptic neuron indirect
Amphetamine and ephedrine
Synapse release agent
Direct acting
On post synaptic neuron