Pharmacology Flashcards
post-ganglionic parasympathetic fibers release _____
Acetylcholine
post-ganglionic sympathetic fibers release ____
Norepinephrine
Chromaffin cells release ________
catecholamines: Epi+Norepi
(~80% Epinephrine ~20% Norepinephrine)
Chromaffin cells are stimulated by the (sympathetic/parasympathetic) nervous system
sympathetic
Classically, Preganglionic sympathetics release ________, and post ganglionic sympathetics release _______
Preganglionic symps: Acetylcholine
Postganglionic symps: Norepinephrine
Classically, Preganglionic parasympathetics release ________, and postganglionic parasympathetics release _______
Preganglionic parasympathetics: Acetylcholine
postganglionic parasympathetics: Acetylcholine
Sympathetic output is generally (discrete/diffuse) while parasympathetic output is (discrete/diffuse)
sympathetic: diffuse
parasympathetic: discrete
Exceptions: for renal vessels, Pregang symps release ________, and postgang symps release _______
Preganglionic symps: Acetylcholine
Postganglionic symps: Dopamine!
Which is degraded rapidly once released from a nerve terminal? (NE/ACh)
ACh
Name 2 drugs that inhibit NE re-uptake:
- Cocaine
2. Tricyclic antidepressants, TCAs
How does botulinum toxin work?
Blocks ACh release
Why is an Nn receptor a bad target for ANS drugs?
It is in both the Symp and Parasymp systems!
M1, M3, M5 are all (Gq/Gi/Gs) coupled
Gq, (increase IP3, Ca2+, DAG)
M2, M4 are (Gq/Gi/Gs) coupled
Gi (decrease cAMP)
Gs, stimulatory proteins (increase/decrease) cAMP
increase cAMP
Gi, inhibitory proteins (increase/decrease) cAMP
decrease cAMP
methylene chloride is dangerous b/c is it converted to ___ in vivo
CO
CO can inhibit the mitochondrial enzyme ________ ________
cytochrome oxidase
CO can displace nitric oxide from _______
platelets
“Late” effects of CO exposure is likely due to a ______ injury
Reperfusion
A Pulse oximeter (can/cannot) tell the difference between blood O2 and blood CO
cannot!
both cause the same change in the iron centers
to accurately measure the blood CO2 you have to use a ________
CO-oximeter
Treatment for CO poisoning is ______
100% O2 or hyperbaric O2
The chemical name for the drug “poppers” is _______
amyl nitrite
Cyanide inhibits the enzyme ________
cytochrome C oxidase a3 (at step 4)
The new cyanide antidote is _________
hydroxocobalamin
Methylene blue is the co-factor for ________ _______
NADPH reductase
methemoglobin reduction to Fe2+
The old cyanide antidote is ________
sodium nitrite
The chemical name for “poppers” is _______
amyl nitrite
use of amyl nitrate can turn hemoglobin to _______
methemoglobin
What is the antidote for a methemoglobinemia?
Methylene Blue
Methylene blus is the co-factor for ________ _______
NADPH reductase
methemoglobin reduction to Fe2+
in methemoglobin, iron is in the _____ state
Fe3+
A patient with methemoglobinemia and with a deficiency in _______ will not respond well to methylene blue
G6PD
How many types of muscarinic receptors are there?
5: M1, M2, M3, M4, and M5
Which Muscarinic receptor is predominant in slowing heart rate?
M2
Which Muscarinic receptor is common in the exocrine glands, blood vessels and smooth muscle?
M3
Which Muscarinic receptor is predominant in creating myosis of the eye?
M3
muscarinic receptors respond to release of (Epi/Norepi/ACh)
ACh
Which Muscarinic receptor is predominant in bronchoconstriction?
M3
What enzyme is inhibited by INDIRECT acting cholinomimetics?
acetylcholine esterase
Drug: Direct-acting muscarinic cholinomimetic for Post-operative and neurogenic ileus and urinary retention
Bethanechol
What makes Inocybe genus and Clitocybe genus of mushrooms toxic?
too much muscarine
Drug: Direct-acting muscarinic cholinomimetic for Glaucoma (ACh activates sphincter and ciliary muscles of eye
Pilocarpine
Drug: Direct-acting muscarinic cholinomimetic for Dry mouth Esp. Sjogren’s (and post- radiation therapy) increased salivation
Cevimeline
Drug: ACh esterase inhibitor, a volatile nerve gas
Sarin
Drug: ACh esterase inhibitor, an insecticide
Parathion
Drug: ACh Esterase inhibitor, covalently carbamylates AChE, for myasthenia gravis and Post-op and neurogenic ileus; urinary retention
Neostigmine
If you are exposed to Sarin gas what you like be be given quickly before irreversible aging?
Pralidoxime
In myasthenia gravis, muscle weakness is caused by ________ that block acetylcholine receptors
auto-immune antibodies
What are the SLUDGE side effects that result from too much cholinergic stimulation?
Salivation Lacrimation Urination Defication GI distress Emesis
Which 2 drug classes have the SLUDGE effects?
- Muscarinic cholinomimetics
2. AChE inhibitors
Drug: AChE inhibitor for Alzheimer’s (amplifies endogenous ACh in brain)
Donepezil
2 drugs: indirect acting AChE inhibitor for Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
- Physostigmine (short acting)
2. Echothiophate (long acting)
Too much neostigmine can lead to flooding the ACh and paralysis. What do you use to check the effect of the neostigmine?
Edrophonium
List the tertiary amine, anti-muscarinics (9) which generally block muscarinic function
Eye: 1. Atropine 2. Tropicamide CNS: 3. Benztropine 4. Scopolamine Bronchi: 5. Ipratropium 6. Tiotropium GI: 7. Glycopyrrolate 8. Dicyclomine GU: 9. Tolterodine
Paralysis of the ciliary muscles of the eye is called _______
cycloplegia
Parasympathetic innervation drives pupillary (constriction/dilation)
constriction
Sympathetic innervation drives pupillary (constriction/dilation)
dilation
Mydriasis is (constriction/dilation) of the pupil
dilation
A muscarinic antagonist (promotes/ inhibits) sweating
inhibits! (receptors are muscarinic cholinergic)
Drug: Tertiary amine, anti-muscarinics
Targets CNS For parkinson’s, penetrates BBB
Benztropine
2 Drug: Tertiary amine, anti-muscarinics
For Mydriasis and cycloplegia
- Atropine
2. Tropicamide
Drug: Tertiary amine, anti-muscarinics
Targets CNS for Prevention or reduction of motion sickness, penetrates BBB
Scopolamine
2 Drugs: Tertiary amine, anti-muscarinics
Target G.I. tract to reduce transient hypermobility
- Glycopyrrolate
2. Dicyclomine
Drug: Tertiary amine, anti-muscarinics
For postoperative bladder spams, incontinence
Tolterodine
2 Drug: Tertiary amine, anti-muscarinics
For bronchidilation in asthma, COPD
- Ipratropium
2. Tiotropium
Two ganglion blockers that block Nn receptors and sympathetic tone are
- Hexamethonium
2. Mecamylamine
What are 1. Hexamethonium and 2. Mecamylamine used for?
“Bloodless” field surgery, the ganglionic blockers decrease blood pressure
Two neuromuscular drugs that are non-depolarizing blockers at Nm junctions are:
- Tubocurarine
2. Mivacurium
When succinylcholine is administered, it causes initial (paralysis/ fasciculations) followed by (paralysis/ fasciculations)
Produces initial fasciculations and then paralysis within 1 minute.
What do 1. Tubocurarine and 2. Mivacurium do?
Block Nm receptors, skeletal muscle relaxation during surgery or mechanical ventilation
Accommodation of the eye is purely under (sympathetic/parasympathetic) control
parasympathetic
Blurred vision is a mark of a (muscarinic/ adrenergic)
muscarinic
To look in someone’s eye, dilate it with (Atropine/Tropicamide)
Tropicamide, dialates eye for less time than
Atropine
To treat parkinson’s use (Benztropine/Scopolamine)
Benztropine
To reduce motion sickness use (Benztropine/Scopolamine)
Scopolamine
To treat cholinergic poisoning like muscarine from mushrooms use _______
Atropine
Cholinesterase inhibitors are used to reverse the effects of (depolarizing/ non-depolarizing) blockers
non-depolarizing
Botulinum toxin as botox is used to (block/ cause) muscle tone
blocks muscle tone: relaxes
The synthesis of Norepiniphrine begins with (arginine/ /Dopamine/ tyrosine/ DOPA)
Tyrosine -> DOPA -> dopamine -> N.E.
The effects of N.E. at a neuron are stopped by the action of the (uptake 1/ uptake2) transporter
uptake 1
N.E. is destroyed in the cell by (acetylcholine esterase/ mono amine oxidase/ PNMT)
MAO on the mitochondria
which is a neurotransmitter (N.E./ Epi)
N.E.
Which is a neurohormone (N.E./ Epi)
Epi
Which adrenergic receptor causes sm. muscle contraction including vasoconstriction(α1/ α2/ β1/ β2/ β3/ D1)
α1
Which adrenergic receptor causes increased heart inotropy (α1/ α2/ β1/ β2/ β3/ D1)
β1
Which adrenergic receptor causes sm. muscle relaxation including arteriole dilation(α1/ α2/ β1/ β2/ β3/ D1)
β2
Which adrenergic receptor inhibits neurotransmitter N.E. release (α1/ α2/ β1/ β2/ β3/ D1)
α2
Which adrenergic receptor causes lipolysis (α1/ α2/ β1/ β2/ β3/ D1)
β3
Which adrenergic receptor causes bronchiole relaxation (α1/ α2/ β1/ β2/ β3/ D1)
β2
Which receptor causes renal, mesenteric and cerebral arteriole dilation? (α1/ α2/ β1/ β2/ β3/ D1)
D1, dopamine as neurotransmitter
Phenylephrine is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 agonist
treats nasal congestion, and postural hypotention
Prazosin is an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 antagonist
treats primary hypertension and BPH
Clonidine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α2 agonist in CNS
treats Hypertension; shock; withdrawal from drug dependence
Fenoldopam is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
D1 agonist
Increases blood flow at renal, mesenteric, and cerebral arteries
Dobutamine is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1, agonist
treats Cardiac decompensation; shock; heart block
Atenolol and Metoprolol are both (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 antagonists
They treat HTN, Angina, Arrythmias, CHF
Albuterol and terbutaline are a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β2 Agonist
Albuterol: bronchospasm; mild asthma; COPD
Terbutaline: above + prevents premature labor
Isoproterenol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 and β2 agonist, non-selective
used to treat shock and heart block
Propranolol is a (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
β1 and β2 antagonist, non-selective
use to treat Angina, Hypertension and Arrythmias
With low concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle
β2, dilation
with low epi
fight or flight
With high concentration of epinephrin at muscles, the (α1/β2) receptor trumps leading to (dilation/ contraction) of vascular smooth muscle
α1, contraction
raises B.P.
Increases release of cytoplasmic N.E. (cocaine/ tyramine)
tyramine
similar to amphetamine
Prevents N.E. re-uptake (cocaine/ tyramine/ amphetamine)
cocaine
short term tolerance is called ________
tachyphylaxis
increased blood flow at renal, mesenteric and cerebral vasculature (low dose/ medium dose/ high dose) Dopamine
low dose dopamine
has direct heart β1 inotropy effects and indirect release of N.E. (low dose/ medium dose/ high dose) Dopamine
medium dose dopamine
has direct α1 vascular effect and indirect N.E. release causing vasoconstriction (low dose/ medium dose/ high dose) Dopamine
high dose dopamine
acts at the D1 receptor only, increases renal blood flow (Dopamine/ Fenoldopam)
Fenoldopam
With bolus N.E.
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. decreases due to vagal feedback
B.P. increases α1 constriction
TPR increases α1 constriction
With bolus epinephrine
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. increases β1 increases inotropy
B.P. increases β1 increases inotropy
TPR decreases β2 sm. muscle dilation
With bolus isoproterenol
H.R. (increases/decreases)
B.P. (increases/decreases)
TPR (increases/decreases)
H.R. increases due to β1 + feedback
B.P. decreases β2 sm. muscle dilation
TPR decreases β2 sm. muscle dilation
epi pens are used for anaphylaxis for their action on (α1/ α2/ β1/ β2/ β3/ D1) receptors
B2, for bronchodilation
For control of post-partum bleeding, and alpha agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergonovine
For control of acute migraines, both and alpha agonsit and a 5HT agonist (Ergonovine/ Ergotamine/ Bromocriptine)
Ergotamine
For control of parkinsons and hyperprolactenemia (Ergonovine/ Ergotamine/ Bromocriptine)
Bromocriptine, a dopamine agonist
Which CNS α2 agonist is a pro-drug? (clonidine/ α-methyl dopa)
α-methyl dopa
crosses BBB
Both treat hypertension, which treats drug dependance (clonidine/ α-methyl dopa)
clonidine
Which β2 agonist is better for asthma? (terbutaline/ albuterol)
albuterol
Which β2 agonist relaxes the uterus to prevent pre-mature labor? (terbutaline/ albuterol)
terbutaline
β2 agonist terbutaline and albuterol will cause (vasoconstriction/ vasodilation)
vasodilation
Non-selective β1+β2 blocker, first generation
Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol
Propranolol and Timolol
β1 selective blocker, second generation (Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Metoprolol + Atenolol + Bisproprolol
Non-selective β1+β2 blocker, also blocks α1, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Labetalol and Carvedilol
β1 selective blocker, plus Ca2+ channel blocker, third generation
(Propranolol + Timolol/ Labetalol + Carvedilol/ Metoprolol + Atenolo + Bisproprolol/ Betaxolol)
Betaxolol
Why use 2nd or 3rd gen beta blockers in pts. with heart failure?
protect against sympathetic drive
Beta blockers are partial “contraceptives” due to their side effect of _______ ______
sexual dysfunction
Phentolamine and Phentoxybenzamine are an (agonist/antagonist) of (α1/ α2/ β1/ β2/ β3/ D1)
α1 and α2 antagonist
for Pheochromocytoma, Raynaud’s and frostbite
Which is better treated with an alpha blocker? (athlosclerotic dz./ vasospastic dz)
vasospastic, such as Raynaud’s
postural hypotension is associated with (α blockers/ β blockers)
α blockers
Which nerve ending blocker prevents synthesis of N.E.
α-methyltyrosine/ reserpine/ guanethidine
α-methyltyrosine
Which nerve ending blocker prevents the packaging of N.E.
α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
Which nerve ending blocker can be used for hypertension
(α-methyltyrosine/ reserpine/ guanethidine
reserpine and guanethidine
Which nerve ending blocker stops the vesicular transporter of N.E. leading to empty vesicles
(α-methyltyrosine/ reserpine/ guanethidine)
reserpine
Which nerve ending blocker is preferentially packaged into vesicles, blocking N.E. transport
(α-methyltyrosine/ reserpine/ guanethidine)
guanethidine
What are the anti-malarial quinolone drugs?
- Quinine
- Chloroquine
- Hydroxychloroquine
- Mefloquine
- Primaquine
Why do anti-malarials go the the parasite’s food vacuole?
ionic drug trapping. antimalarials are weak bases.
which is a anti-malarial folate inhibitor? (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Chloroguanide
Which depolarizes malarial parasite mitochondria and inhibits electron transport? (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Atovaquone
Which anti-malarial inhibits the parasite’s sarco/endoplasmic reticulum Ca2+ ATPase SERCA (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Artesunate
Which antimalarial oxidizes the malaria schizont membrane? (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Primaquine
Which antimalarial should NOT be used with G6PD deficiency? (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Primaquine
For uncomplicated malaria, treat with (Quinine/ Chloroquine/ Hydroxychloroquine/ Mefloquine/ Primaquine)
- Chloroquine
2. Hydroxychloroquine
For Chloroquine resistant P. falciparum treat with (Mefloquine/ Primaquine/ Atovaquone-proguanil/ Chloroguanide/ Artesunate)
Atovaquone-proguanil
For Radical cure of persistent malaria use (Mefloquine/ Primaquine/ Atovaquone/ Chloroguanide/ Artesunate)
Primaquine
Antihistamine “cold” medication that is non-sedating (promethazine/ chlorpheniramine)
chlorpheniramine
Non-sedating antihistamines Claritin and and Allegra are ________ and ________
loratidine and fexofenadine
An antihistamine that is both sedating and antiemetic (promethazine/ chlorpheniramine)
promethazine
An antihistamine that is anti-motion sickness (loratidine and fexofenadine/ meclizine and hydroxyzine)
meclizine and hydroxyzine
First line treatment for allergic rhinitis are _______ and _______
azelastine and cetirizine=zyrtec
What are the 4 histamine H2 blockers?
- cimetidine
- ranitidine
- famotidine
- nizatidine
Which H2 blockers has the least side effects?
cimetidine/ ranitidine/ famotidine/ nizatidine
nizatidine
What liver enzyme do the H2 blockers, cimetidine + ranitidine, inhibit that leads to their bad side effects?
CYP 450
therefore are liver toxic
Serotonin blocker used to treat carcinoid syndrome with diarrhea (cyproheptadine/ ondansetron or granisetron)
cyproheptadine
Serotonin blocker used to treat chemotherapy induced nausea and vomiting (cyproheptadine/ ondansetron or granisetron)
ondansetron or granisetron
A 23 year old woman has psoriasis affecting 10% of her BSA. What should you treat her with? (a biologic/ methotrexate/ a retinoid)
a biologic, infliximab
MTX and retinoids could be bad for fertile women
A 45 year old man has psoriasis covering 45% of his BSA what shoud you treat him with? (a biologic/ methotrexate/ a retinoid/ tpoical therapy)
MTX
45% of BSA it too much for a topical alone
What is the role of TNF-alpha in psoriasis?
inflammatory