Pharmacology Flashcards
What are the first and second line treatments for Generalized Anxiety Disorder?
1st line: CBT and/or SSRIs or SNRIs
(this is helpful because depression is often a co-morbid condition)
2nd line: benzodiazepines (diazepam, clonazepam, etc.) These are less desirable due to their risk of tolerance and dependence.
How do sulfonylureas work in diabetes patients to release insulin?
Sulfonylureas bind to ATP-sensitive K channels and cause their closure independent of ATP (ATP is typically generated by glucose entering the cell and generating ATP).
K channel closure -> Ca channel open -> increased intracellular Ca -> insulin release
What is the longterm treatment for Myasthenia Gravis?
Pyridostigmine (AchE inhibitor ) -> outcompetes the inactivated nicotinic receptors (by MG Abs) at the motor end plate.
Occasionally neostigmine is also used.
What is a tensilon test? What do positive and negative test results indicate?
In Myasthenia Gravis patients who are showing symptoms, give them EDROPHONIUM to transiently reverse symptoms (indicating an undertreated MG patient, a POSITIVE test) OR to worsen symptoms briefly (indicating a cholingeric crisis, a NEGATIVE test).
What are nondepolarizing neuromuscular blockers? How do they work? What can be used to overcome them?
Tubocurarine
Pancuronium
Cisatracurium
(CURARE)
Work by inhibiting the nicotinic (which binds Ach) receptors at the NMJ
THEREFORE: AchE inhibitors (i.e. -stigmine) drugs can be used to reverse them
What is a depolarizing neuromuscular blocker? How does it work?
Succinylcholine. Actually is a nicotinic receptor agonist. The hyperstimulation in phase 1 maintains the muscle as chronically depolarized and thus unresponsive to further impulses.
Which Acetylcholinesterase inhibitor has central (i.e. can cross CNS) effects? What is it used for?
Physostigmine
Used to reverse atropine/Jimson weed poisoning.
What are organophosphates?
Nerve gas and insecticides (e.g. -thiols/thions) that act as acetylcholinesterase inhibitors
What are the treatments for organophosphate/insecticide poisoning?
Pralidoxine for peripheral effects:
Regenerates acetylcholinesterase at muscarinic and nicotinic receptors (reversing DUMBBELLS). Does NOT reverse flaccid paralysis (i.e. Central CNS effects).
Atropine can reverse central and peripheral effects.
What are the alpha 2 agonists? What do they do?
Clonidine
Act as centrally-acting sympatholytics. Useful in hypertensive emergencies, ADHD, and Tourettes
Alpha-methyldopa
Act as a centrally-acting sympatholytic
Used to treat HTN in pregnant women
Tizanidine
Centrally-acting muscle relaxant
What are the alpha (1 and 2) antagonists?
Phentolamine reversible
Lowers peripheral vascular resistance via vasodilation, reduces BP
Phenoxybenzamine irreversible
Mirtazapine (2 only) - atypical depression med
What drug is useful in treating cocaine toxicity? What drug should specifically NOT be used?
Phentolamine - alpha antagonist
Beta blockers should NOT be used because they would leave unopposed alpha vasoconstriction
Prior to surgery for removal of a pheochromocytoma, patients are given ________ several days in advance and _____ intraoperatively because they are both alpha blockers and maintain vasodilation/low BP.
Phenoxybenzamine in advance - it is irreversible
Phentolamine intraoperatively - reversible
Alpha 1 receptors are located ______.
Alpha 2 receptors are located ______.
Alpha 1 = peripherally
Alpha 2 = peripherally AND centrally
What are the Alpha 1 selective antagonists? What are they used for?
-“osin” drugs:
Prazosin
Terazosin
Doxazosin
Tamsulosin
Used to treat the symptoms of BPH by relaxing smooth muscle of the urethra and prostate.
Prazosin - PTSD
What are the beta 1 selective beta blockers?
A-M drugs
Atenolol Betaxolol Esmolol Acebutolol Metoprolol
What are the non-selective beta antagonists that also have alpha 1 blocking ability?
Carvedilol
Labetalol
_____ inhibition at the JGA reduces renin production, ultimately reducing BP.
Beta 1
Acute treatment of aortic dissection includes giving IV ______s such as ______.
Beta blockers
Labetalol
Esmolol
Propranolol
What cardiac drug class can be used as prophylaxis for migraines?
Beta blockers
First line treatment for essential tremors is _____.
Beta blockers
What is a non-selective beta blocker?
Propranolol
What curious tx is given for beta blocker overdose?
Glucagon
How do vincristine and vinblastine work?
They bind to tubulin building blocks and preventing their polymerization preventing microtubule production/mitotic spindle formation -> cell death
What are the toxicities/side effects of vincristine (and other anti-microtubule drugs)?
Peripheral sensory neuropathy - stocking glove
Autonomic nervous system dysfunction -> paralytic ileus
Alopecia
What are the toxicities/side effects of vinblastine and taxanes?
Myelosuppression
How do the “taxanes/taxel” drugs work?
Stabilize microtubules and promote their assembly ultimately leading to cell death.
What are the tyrosine kinase inhibitors? (suffix and examples) What is the sketchy scene?
-“nib”
Imatinib Erlotinib Sorafenib Sunitinib Vemurafenib
Sketchy scene = signing of the declaration of independence
Imatinib = tx for ____ and ____.
Receptor tyrosine kinase inhibitor
Imatinib = Gleevec ->Tx for CLM bcr/abl t(9;22)
AND
C-kit GIST tumors (GI stromal)
What is the mechanism of Rituximab?
Binds to CD20 on B cells inducing apoptosis.
What is serum sickness?
A delayed (Type III) immune reaction after infusion of a chimeric monoclonal ab. Characterized by fever, rash, lymphadenopathy, proteinuria, etc. Generally occurs 7-10 days after infusion.
Occurs due to the human immune system reacting against the mouse portion of the Ab.
Tx = steroids
Triptans (e.g. sumatriptan) are what kind of drug used to treat what?
Serotonin 5-HT1b/1d agonists which counter the pathophysiologic mechanisms of migraine headaches by inhibiting release of vasoactive peptides, promoting vasoconstriction and blocking pain pathways in the brainstem.
They are used for the ACUTE and ABORTIVE (i.e. not prophylactic) treatment of migraines.
Why does propofol have such a rapid onset followed by a rapid reversal?
Initial onset is rapid because it is lipophilic and will quickly go to/enter organs receiving high blood flow.
It subsides quickly as blood is redistributed and thus the drug is redistributed all over the body and can sit in adipose tissue, muscle, etc.
______, a depolarizing NMB, is used for rapid-sequence intubation.
Succinylcholine
What is the difference between propranolol and metoprolol?
Propranolol is a non-selective beta blocker
Metoprolol is beta 1 selective
Which classes of antiarrhythmics can cause QT prolongation/torsades de pointes?
Class IA (quinidine, procainamide) and Class III (amiodarone, dofetilide, sotalol)
After administration of corticosteroids, on CBC you will see _____philia due to what?
Neutrophilia as neutrophils “demarginate” aka leave their posts on endothelial cells. Free circulation however means they are sub-functional and thus this is one of the factors in immunosuppression secondary to corticosteroid administration.