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Case Files Questions pharm block II
Questions based on some of the Case Files aligned with this block's material
Terms in this set (69)
Characterized by feelings of intense muscle restlessness or strong desire to move about, usually during the first 2 weeks of treatment with an antipsychotic medication = ?
aliphatic, piperidine, and piperazine are all subsets of which class?
Which receptors are acted on by antipsychotics?
Postjunctional D2, 5HT-2a, mostly dopamine in mesocortex and mesolimbic sys
Haloperidol-induced Parkinson syndrome is a result of haloperidol's action on which tract?
Nigrostrital - Duh, Parkinsons
The therapeutic effect of haloperidol is mediated, at least in part, by its blockade of which receptors?
What side effect is more likely with haloperidol than with phenothiazines? What are MC Ses with the phenothiazines?
Dystonia, akathisia, and Parkinson syndrome-- low-potency phenothiazines = more likely to cause autonomic problems
Which heterocyclic is contraindicated in seizure pts
What drug is famous for its interactions with tyramine
Phenelzine-- an MAO-I
Which P450 isoform is inhibited by Fluoxetine?
The antidepressant action of imipramine is thought to be caused by which MOA
Imipramine is a TCA-- work via Blockade of prejunctional neuronal norepinephrine and serotonin uptake transporters in CNS
What drug besides Lithium is indicated for treatment of BPD
the antiepileptic drugs valproic acid and carbamazepine, and the antipsychotic agent quetiapine are also first-line drugs
The therapeutic action of Li+ is thought to be caused by direct inhibition of?
Will diuretics increase renal clearance of Li? If not, what will?
Pregnancy-- diruetics that result in hyponatremia will often decrease its clearance
What are the MC Side effects of lithium at therapeutic dose?
GI effects, polydipsia --> polyuria, and hyPOthyroid
What is the MoA of L-dopa?
L-dopa is decarboxylated in the prejunctional CNS neurons to restore dopamine in the corpus striatum
Why is L-dopa given with Carbidopa?
Carbidopa inhibits peripheral but not central dopa-decarboxylase metabolism of l-dopa
What is MC side effect of l-dopa
Involuntary dyskinesia (90%), also behavioral effects like depression, insomnia, nightmares, changes in mood
What Parkinson drugs cause orange discoloration of the urine?
COMT Inhibitors -- Remember that Tolcapone can be hepatotoxic as well
What Parkinson drug causes livedo reticularis?
Which Parkinson drug can cause serotonin storm if mixed with an SSRI or TCA or Meperedine?
Selegiline or Rasagiline
Furosemide acts to inhibit Na+ reabsorption in which of the following locations?
Ascending limb of LoH-- specifically on Na/K/2 Cl- tritransporter
A patient arrives in the emergency room in a coma and has a serum Ca2+ of 4.5 mM. You start a saline infusion of which of the following drugs?
A loop diuretic-- Ethacrynic acid, for instance, will increase excretion of Ca2+
What electrolyte imbalance goes w Furosemide?
Furosemide leads to hypokalemia, hypomagnesemia, and metabolic alkalosis (inc bicarb)
What is used to manage these electrolyte disturbances (w Furosemide)
potassium-sparing diuretics such as triamterene or spironolactone
What is the MOA of Probenacid
Inhibits secretion of organic acids, decreases reabsorption of uric acid
What drugs whose secretion is inhibited by Probenacid
Pennicillin, indomethacin, methtrexate
What transporters lead to the secretion of urate?
OAT-1 and OAT-3, which exchange a-ketoglutarate and urate
What needs to be given concurrently with probenacid to prevent acute gouty attack
Water-- hydration is important
What common drug is contraindicated in pts on probenacid
Aspirin-- will compete for secretion
What is the combo often used for gonhorrea?
Probenacid + Pennicillin-- former increases half-life of the latter
Morphine produces analgesia through which of the following actions?
D. Reduction of prejunctional neuronal calcium conductance, via a G-protein coupled receptor to reduce adenylyl cycalse activity.
Which opioid agonist is NOT metabolized to an active ingredient with analgesic activity?
Meperidine is metabolized to normeperidine that may result in seizures
Why would morphine's activity be accentuated in someone with renal failure?
The active metabolize, morphine-6-glucuronide
How do BZs work?
Bind to a distinct BZ receptor on the GABA receptor to allosterically increase the affinity for/frequency of interactions of GABA with GABA-a receptors.
What is used to rx BZ overdose?
Flumazenil-- a competitive antagonist at BZ receptors.
Which BZ is metabolized to a long-acting active metabolite in the gut?
Clorazepate, which gets decarboxylated to the 50 hour half-life drug N-desmethyldiazepam.
Which becoming-more-common condition due to obesity is a contraindication for BZ?
What is the main rationale for use of BZ in management of detoxing alcoholics?
Cross-tolerance-- both work with GABA-A receptor, therefore a long-acting BZ can be used to ameliorate sx associated with EtOH withdrawal
Which BZ is indicated in status epilepticus?
What is the MoA of Lidocaine?
Time and voltage-dependent blockade of the inactivated Na+ channels on the inner axon membrane
Why would you want to treat an infection before giving a local anesthetic?
Infections or inflammation lower tissue pH, which reduces the diffusion of a local anesthetic into the nerve (by protonating the weak base anesthetic, which makes it a cation and therefore unable to cross the membrane), thereby reducing its effectiveness
What sort of change in the length of a carbon chain on a amide anesthetic would increase the T1/2 and the potency?
Lengthening it. Therefore bupivacaine (butyl) >> mepivacaine (methyl) in terms of both.
Which local anesthetic can result in methemoglobinemia?
Prilocaine, which gets metabolized to o-toluidine
Why are ester anesthetics short acting?
Hydrolyzed in blood by circulating butyrlcholinesterase
Which fibers get blocked first?
Thin fibers with high firing rates that are myelinated. In practice, C Type fibers.
What is EMLA?
A topical mix of lidocaine and prilocaine, used to anesthetize skin primarily in peds
Local anesthetic action is a result of blockade of the movement of which of the following ion channels?
An allergic reaction is most likely to occur with which of the local anesthetics?
The esters (e.g. Procaine), which are metabolized to form the allergen para-aminobenzoic acid
What are reasons epinenephrine is combined with locals for injection?
Prevent distirbution from site of action, also control bleeds
How are amide anesthetics metabolized?
At various rates by hepatic microsomal enzymes-- therefore in liver disease pts, toxicity is more likely, or when combined with P450-using drugs, half-life may increase
What can be done to a SOLUTION of a local anesthetic to accelerate the onset?
Carbon dioxide saturation
What are signs of systemic local anesthetic toxicity, particularly with lidocaine?
Neurotoxicity, including nystagmus, switching, tonic-clonic seizures, respiratory depression
What anesthetic can lead to liver toxicity?
Halothane, in about 25%
Which general anesthetic has an unpleasant odor and a short duration of action?
How does MAC relate to potency?
Low MAC -> High potency
What property of an anesthetic has the most to do with time of onset?
Blood and tissue solubility-- low solubility = faster time to blood/brain equilibration
What is the relationship between MAC and rapidity of onset?
Why are benzos used to rx alcohol withdrawal?
What DRUGS can be used to manage alcoholism?
Disulfiram and Naltrexone
Second generation anti-histamines are selective for which receptor?
Site of action of sumatriptan?
5HT-1D and 1B
How does sumatriptan work at a molecular level
Inhibits adenyl cyclase, decreases cAMP leading to vasoconstriction
Which drugs are associated with the SE of prolonged vasospasm?
What drug can be used that works on a-adrenceptors, causing contraction of uterine muscle?
Which drugs can be used for prophylaxis of migraine?
Methysergide-- antagonist of 5HT vasoconstriction. Blocks 5HT2A, C
What is a bad SE of Methysergide?
Which prostaglandins contract uterine smooth muscle
Which prostaglandins are vasodilators, which are constrictors?
I and E are dilators, F is constrictor
Which anti-inflammatory has the highest incidence of adverse effects
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