Card Set Information
2 Acidic drugs?
2 basic drugs
2 Ach agonists used for Glaucoma
: ciliary muscle contraction--- increase outflow thru the canal of schlemm
2 Beta antagonists used for Glaucoma
: block NE at ciliary epithelium--decrease aqueus humor formation
Ach esterase inhibitor?
: increase outflow
Sympathomimetic drug for Glaucoma?
Apraclonidine Apha 2 agonist--
: deacrease NE realease at the presynaptic junction
: increase OUTflow
Carbonic anhydrase inhibitor for Glaucoma?
Acetozolamide, Dorzolamide--decreases HCO3 formation leading to deacreased Acqueus humor formation
PGF2 apha analog for Glaucoma?
Inhibitor of choline at the nerve ending?
ACh antagonists used for Asthma?
MOA of Botulinum toxin?
inhibits Ach release from the presynaptic membrane
What receptors signal thru the q arm of the G protein?
What is the signalling cascade for the q arm of the G protein?
+ phospholipace c--- + IP3--- +Ca
--- + DAG---- + Protein Kinase C
What receptor signal thru the inhibitory arm of the G protein?
M2, Apha2, D2
What is the signalling cascade of the Inhibitory arm of the G protein?
--- -AC----- -cAMP ----- -Protein Kinase A
What receptors signal thru the stimulatory arm of the G protein?
Beta1, Beta2, H2,V2, D1
What is the signalling cascade of the stimulatory arm of the G protein?
--- +AC---- + cAMP ---- +Protein Kinase A
Antidote for Heparin toxicity?
Antidote for warfarin Toxicity?
Fresh Frozen Plasma
Warfarin inhibits synthesis of what clotting factors?
2,7,9,10, protein C, Protein S
Heparin inhibits the synthesis of what clotting factors?
7, 9, 10, 11, 12
Antidote for cholinesterase inhibitor poisoning?
atropine + pralidoxime (regenerates AchE)
Irriversible acetylcholine esterase inhibitor?
cholinestarase inhibitor used for Urinary Retention?
Cholinestarase inhibitor used for glaucoma?
Ach agonist used for asthma diagnosis?
MG diagnosis (short acting cholinesterase inhibitor)
Ach agonist used for MG (long lasting)
Insecticides contain what 2 acetycholine esterase inhibitors?
2 acetylcholine esterase inhibitors used for Glaucoma?
What are the effects of acetylcholine inhibitor poisoning?
Excitation of the CNS
Nicotinic receptor agonist?
Muscarininc receptor direct agonists?
Bethanecol is used for activation of what?
Nn receptor antagonist?
Nm receptor antagonist?
Benztropine used for what?
Parkinsons--PARK my BENZ
Scopolamine used for what?
Ach antagonist used for asthma?
Nicotinic receptor stimulation at the adrenal Medulla causes what?
release of epi and Norepi
Nicotinic stimulation at the autonomic ganglia causes what?
Nicotinic stimulation at the NMJ causes what?
sk. muscle contration
Ach at the Nn and Nm signalls how?
What 2 effects does Ach have on the eye?
sphincter muscle contraction
ciliary muscle contraction
What effect does ach have on the SA and AV node?
SA node--decreases stimulation
AV node--decreases conduction velocity
What effect does Ach have on the purkinje fibers and ventricles?
Where is M1, M2, M3 found in?
M1---GI glands and CNS
M3--Lungs, GI, GU, Glands, BV
What effect does M3 receptor binding of Ach have on the bladder?
Detrusor muscle and sphincter stimulation
What are the 7 different locations for Ach receptors in the body
2. sweat, lacrimation, gland secreations
Tx for ileus and urinary retention?
Diagnosis of bronchial Hyperactivity?
Ach agonist treatment for glaucoma?
Ach agonist Tx for Xerostomia?
What acetycholine esterase is used for atropine overdose?
What ach agonist and acetylcholine esterase inhibitor is used for ileus and urinary retention?
Reversal of nondepolarizing NM blockers i.e tuburocurarine, atriacurium, succinylcholine
acetylcholinesterase Inhibitors used for Alzeimers?
Acetycholine esterase inhibitor used for Glaucoma?
irriversible acetylcholine esterase inhibitors?
ecothiophate, malathion, parathion
What drugs are contraindicated in Glaucoma?
Atropine O'D is treated with what acetylcholine estersase inhibitor?
What is given during anesthesia to block bradycardia?
anticholinergic i.e atropine
Tropicamide, Atropine, Homatropine produce what effect?
Glycopyrrolate is used for what?
peptic ulcer treatment, antispasmodic
Trihexphenidyl, benztropine are used for what?
In dually innvervated organs, which arm of the ANS predominates and is thus blocked?
Where is sympathetic activity predominant and thus blocked?
What effect would a nicotinic antagonist such as hexamethonium have on
What effect would hexamethonium have on
Veins--dilation, decreased venous return
What are 2 ganglionic blockers?
Tx for malignant hyperthermia?
Ca channel blocker
What does amphetamine do to the slopw of epinephrine?
potentiates it, so it shifts it to the left
What ach agonist is used for the sweat test in CF?
Ach esterase inhibitors have muscarinic effects of muscarinic agonists, except in what location?
BV- bc they are not innervated so Ach esterase is absent , so the drug cannot block it and increase Ach levels
What is a cholinergic crisis?
Nicotinic receptors are desenthysized
How is a cholinergic crisis differentiated from MG?
if endrophonium improves the symptoms then its MG
if endrophonium doesn imporove symptoms--then it is cholinergic crisis
What is the significance of a tertiary and quarternary Ach esterase inhibitors?
tertiary are unionized so cross BBB-CNS effects
Quarternary--are ionized---cant Cross BBB
Antidote for Atropine O'D?
Antidote for depolarizing NMJ drugs i.e tubocurarine, atracurine,
Taking too much of Ach esterase inhibitors can result in what kind of crisis?
Sarin is an example of what type of inhibitor?
non competitive/irriversible cholinesterase inhibitor poisoning
Phosphorylation usually occurs at what aa?
What are the 3 C's of anti-muscariniv O'D?
What are 2 drugs used for motion sickness?
What are the drugs that have anti muscarinic effects?
2 Drugs used for dyskinsia in Parkinsons diseas
What drug prevents conversion of tyrosine to Dopa?
Alpha 2 receptors have what effect on the NE?
inhibits the release of NE
Which receptors are more sensitive to stimulation, alpha or beta?
Indirect sympathomimetic that releases the mobile pool?
Indirect sympathomimetic that blocks NE reuptake?
What 2 receptors block the release of NE from the presynaptic membrane?
What receptor stimulates the release of NE from the presynaptic membrane?
Which MAO metabolizes NE, 5HT and Tyramine?
Which MAO metabolizes Dopamine?
MAO A inhibitors?
MAO B inhibitor?
Selegiline is used for what condition?
What enzyme metabolizes NE and dopamine at the post junctional membrane?
A COMT inhibitor used in Parkinsons?
What drug blocks the reuptake of NE from granular pool?
What drug inhibits the release of NE from the Granule Pool?
Presynaptic alpha 2 agonist?
Alpha 1 receptors are found where?
Veins--constriction--Increased VT/Diastolic pressure
Arteries--constriction--increased TPR/Systolic pressure
Radial muscle of Eye
GI and bladder Sphincter
Decrease Insulin Release
Alpha 2 receptors have what function?
inhibit NE release/anti sympathetic
Beta1 receptors are found where?
Heart-SA, AV node, atria, ventricle, purkinje fibers
Increase Renin release
B2 receptor found where?
Increase Liplysis, glucoenogenesis, Glycogenlysis, insulin
Whats an example of a TOCOlytic Receptor?
Which adrenergic receptor will cause reflex bradycardia?
D1 receptors are found where?
renal artery--vasodilation--maintain GFR
in high conc. acts on B1--incrases contractility and alpha1 increases TPR all raising BP in hypotension
At low does of adrenergic agonist, what receptors are activated?
At high doses?
2 alpha agonists?
Alpha 1 agonist used as a decongestant?
2 alpha 2 agonists
alpha methyl dopa
Beta 2 agonists?
Beta 2 agonist used as a tocolytic?
Dobutamine is more selective for what receptor?
Isoproterenol is specific for what adrenergic receptor?
beta 1 and beta 2
What beta 2 agonist is used for asthma prophylaxis?
What is used for treatment of acute asthma?
Doputamine is used for what?
Norepinephrine is selective for what receptors?
alpha1, alpha2, beta1
What reflex is seen with norepinephrine?
Epinephrine is selective for what receptors?
alpha1, alpha2, beta1, beta2
Epinephrine in low doses is more selective for what receptors?
in large doses?
What reflex is seen with low doses of epinephrine?
no reflex bc beta1 increases HR but beta2 decreases TPR so the actions offset eachother
What is the reflex with large doses of epi?
beta 1 is stimulates so u get increased HR but alpha 1 increases TPR so you get reflex bradycardia
What alpha 1 agonist is used for nasal decongestant?
what is used for paroxysmal atrial tachycardia?
How does epi reversal work?
giving an alpha blocker you go from hypertension to hypotension
What drug produces a hypertensive crisis with MAO inhibitors?
Amphetamines and ephedrine have what effects?
Release of NE from the mobile pool
How does ephedrine produce a decongestant effect?
ephedrine--- + NE-----vasoconstriction via alpha
How does cocaine produce its effects?
blocks reuptake of NE, 5HT, Dopamine
How is cocaine a local anesthetic?
blocks Na+ channels, prevents depolarization
Dopamine at low doses has what effects?
acts on D1 on the kidney, maintainsRBF and GFR
Dopamine at medium levels has what effects?
acts on D1 and Beta1 increases CO
Dopamine at high levels has what effect?
stimulates beta1 and alpha1
Vasoconstriction and increases CO
Alpha agonist that is a nasal decongestant?
Reversible Alpha1 and Alpha2 antagonist?
Irriversible alpha1 and alpha2 antagonist?
Which alpha 1 and 2 antagonist is used in Pheochromocytoma?
Alpha 1 antagonist?
Prazoncin, Doxazocin, Terazocin
Alpha1 antagonist used for BPH?
Alpha 2 blockers?
Yohimbie is used for what?
postural hypotension, impotence
Mirtazapine is used for what?
2 alpha 2 antagonists?
are use for what?
Beta blockers used for Glaucoma?
nonselective beta blocker?
2 Alpha and beta antagonists?
Beta1 cardioselective antagonists?
Beta blocker for CNS depression?
Side effect of propranolol?
increased LDL and TGs
Beta blockers with intrinsic sympathetic activity?
What Beta blockers do not cross the BBB?
How would a beta1 blocker bloc the effects of hypoglycemia?
in hypoglycemia you get tachycardia
with a b blocker the tachycardia stimulus is stopped
Why do you get tachycardia, angina, arrythmias after an abrupt withdrawal of beta blockers?
bc beta receptors are upregulated so they get over stimulated and produce increased sympathetic tone
What stimulants are contra indicated in MAO inhibitor use?
All release NE stored in the Mobile pool
Why do people get perforated nasal septum?
cocaine ---- + NE release + vasoconstriction --+ ischemia ---+ tissue death=perforated septum