Pharm Flashcards

1
Q

Mechanism and side effect of high-potency antipsychotics like haloperidol and fluphenazine.

A

Strongly block D2 receptors and cause extrapyramidal symptoms (due to blocking D2 in the nigrostriatal tract).

Note: muscle spasms, stiffness, tongue protrusions of twisting, oculogyric crises (forced, sustained elevation of the eyes in an upward manner)

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2
Q

Side effect of these types of drugs cause orthostatic hypotension and lightheadedness.

A

Alpha-1 adrenergics

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3
Q

Flumazenil is a GABAa antagonist. What is it used for?

A

Counteracting acute overdosing of benzodiazephines.

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4
Q

What type of drugs are chlorpromazine and clozapine?

A

H1-histamine antagonist–>causes sedation.

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5
Q

Clavulanic acid, sulbactam, and tazobactam are what type of drugs?

A

Beta-lactamase inhibitors, use will penicillins against organisms that produce beta-lactamase (S aureus, H. influenza, Bacteroids, and other gram - bacteria)

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6
Q

Protamine sulfate is used for _______________ toxicity.

A

Heparin

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7
Q

What do you use for reversal of warfarin overdose.

A

Fresh frozen plasma in acute life threatening situations to give the patient clotting factors. Vitamin K can also be given, but it takes time to use.

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8
Q

Clozapine is drug to treat schizophrenia. What is the most common side effect?

A

Granulocytopenia. Need to do CBC regularly.

Acts on D4 receptors and less likely to cause the extrapyramidal problems.

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9
Q

Norepinephrine is given when people are severely hypotensive. It works on alpha receptors (both 1 & 2) and beta 1 receptor.

What is the second messenger for each receptor and when is the clinical effect?

A

Alpha 1: Increased IP3–>peripheral vasoconstriction

Alpha 2: Decreased cAMP—>Decreased release of norepi and insulin

Beta 1: Increased cAMP–>Increased contractility.

Just for reference:
B2: increased cAMP–>bronchodilitation and vasodilation.

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10
Q

The following drugs treat M. tuberculosis:

Isoniazid
Ethambutol
Pyrazinamide
Rifampin

Which one of these drugs requires an acidic pH in order to work?

A

Pyranzinamide (works best at killing organisms engulfed by macrophages.)

The other three work best on extracellular bacteria.

Isoniazid: inhibits synthesis of mycolic acid (cell wall)

Ethambutol: inhibits mycobacterium cell wall synthesis by blocking arabinosyl transferase.

Rifampin: inhibits mycobacterial CNA-dependent RNA polymerase.

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11
Q

What is a rare but very serious adverse effect of ACE-inhibitors (the ‘pril’ drugs)

A

Build up of bradykin (which is a potent vasodilator). ACE typically is responsible for the breakdown of bradykinin.

Bradykinin is a potent vasodilator that ultimately increases vascular permability causing significant ANGIOEDEMA.

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12
Q

Sertraline is an SSRI used to treat depression. What is the most common side effect that limits its use?

A

Sexual dysfunction.

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13
Q

Class of antidepressants that can cause cardiac arrhythmias so are not used very much anymore

A

Tricyclics…like imipramine, doxepin and amitryptaline

Note: TCAs also cause urinary retention, seizures 9(clomiparamine) and orthostatic hypotension, and sedation

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14
Q

Used prophylactically to help deal with cisplatin-based chemotherapy.

A

Amifostine: thiol-based cytoprotective free-radical scavenging agent used to decrease the cumulative nephrotoxicity associated with platinum-containing agents.

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15
Q

Luecovorin

A

Folinic acid: used to treat methotrexate overdose.

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16
Q

Filgrastim

A

G-CSF analog, used to stimulate the proliferation and differentiation into granulocytes.

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17
Q

Fomepizole

A

Used to treat suspected methanol (rubbing alcohol) or ethylene glycol poisoning. Competitive antagonist of alcohol dehydrogenase.

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18
Q

Dexrazoxane:

A

iron-chelating agent that can help prevent anthracycline induced (i.e. doxorubicin) cardiotoxicity (CHF)

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19
Q

What is the main contributor of the effectiveness of nitrates in patients with stable angina?

A

Nitrates act primarily as venodilators causing a decrease in cardiac work by decreasing LEFT VENTRICULAR FILLING VOLUME OR PRELOAD.

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20
Q

Botulinum toxin causes disease by inhibiting cholinergic nerve, classically motor neurons at the neuromuscular junction. HOw does it specifically cause paralysis?

A

It it endocytosed at nerve terminals where it prevents binding and fusion of ACH-containing exocytotic vesicles with the plasma membrane, effectively blocking ACH release into the neuromuscular synapse.

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21
Q

If an individual with tb is taking isoniazid and starts complaining of numbness and tingling in the hands and feet, what the condition most likely caused by?

A

Vitamin B6 deficiency: Isoniazid is chemically similar to pyridoxine (B6), so it competes with the vitamin in synthesis of multiple neurotransmitters (like GABA) which results in defective end products. It also causes B6 to be secreted, creating a deficiency.

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22
Q

HIV drugs that selectively bind to gp41 prevent the virus from getting into the target cell. How so?

A

Prevent the conformational changes necessary for the viral membrane to fuse iwth the target cellular membrane. These agents are known as “fusion inhibitors”.

ENFUVIRTIDE is an example of a fusion inhibitor.

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23
Q

Loss of consciousness brought about by severe hypoglycemia should be initially treated how?

A

Intramuscular glucagon (which will increase hepatic glycogenolysis and gluconeogenesis). Note: if it were in the medical setting, you will do IV dextrose.

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24
Q

Why is active tb never treated with drug mono therapy?

A

The fast emergence of mycobacterial antibiotic resistance from rapid, selective gene mutations.

Isoniazid monotherapy may be used only in a patient who has a positive PPD and negative chest X-ray (no evidence of clinical disease)

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25
Q
What are these clinical features of:
Abdominal cholic
Constipation
Headache
Bluish pigmentation at gum-tooth line.
Peripheral neuropahy
Microcytic hypochromic anemia and BASOPHILIC STIPPLING
A

Lead poisoning.

blue gum line = lead line
colicky abdominal pain = lead colic

26
Q

What agent is suggested to be added to any patient’s regime for CHF?

A

Spironolactone: aldosterone antagonist with mild diuretic effects.

27
Q

Milrinone is a phosphodiesterase isoenzyme 3 inhibitor and is an inotropic agent. What additional response is an extension of the inhibition of this enzyme?

A

Phosphodiesterase isoenzyme 3 is acts to metabolize cAMP in the myocyte. Thus inhibition of PDEI3 by milrinone will cuase increase in cardiac contractility (b/c more cAMP second messenger.

Note: In vascular smooth muscle, cAMP causes VASODILATION via B2 receptors. Also remember that alpha1 receptors, which cause vasoconstriction of smooth muscle uses IP3 as a second messenger.

28
Q

AIDS patients with a low CD4 count (

A

G6PD levels, because dapsone puts oxidative stress on the body. Remember that common precipitating factors of g6PD deficiency are:
1. infections.
2. Drug: dapsone, antimalarials, sulfonamide antibiotics (TMP-SMX)
3. Diabetic ketoacidosis
4 Favism (fava beans)

*Remember, G6PD is important in synthesis of NADPH, which can convert O2-radical to H2O2.

29
Q

What does this sound like:

red cell fragments, microspherocytes, “bite” cells.

A

G6PD deficiency

30
Q

Why would you skip an evening dose every day in a patient who is taking long-term nitrates as part of treatment for exertional angina?

A

Tolerance development.

31
Q

People on opioids rapidly develop tolerance to euphoria, sedation, nausea and vomiting, respiratory depression, cough supression and urinary retention. What do individuals taking opioids NOT become tolerant to? (2 things)

A

miosis and constipation

32
Q

What class of antiarrhythmics will change the QT interval?

A

Class III (block K+ efflux that repolarizes the cardiac myocyte).

Note: amiodoraone, ibutilide, and and dofelide are Class III anti-arrhythmics. Sotalol is a class III that also is a beta blocker, so in addition to a long QT, it will also cause bradycardia.

33
Q

Varapamil and diltiazem are class ____ antiarrythnics.

A

4–Calcium channel blockers.

Verapamil is more cardioselective, but both can work peripherally, which will cause a decrease in blood pressure. Slow the phase 0 depolarization of cardiac pavemakers and phase 2 of myocyte action potential. But neither block QT interval.

Verapamil: side efx–>gingival hyperplasia and constipation

34
Q

This drug can cause hypothyroidism and nephrogenic diabetes insipidus

A

Lithium: used to treat bipolar.

35
Q

Anti-seizure med that is associated with hepatitis and teratogenicity

A

Valproic acid

36
Q

Side effect of fluphenazine

A

It is traditional anti-psycholtic, so it causes extrapyramidal symptoms.

37
Q

Clozapine is an atypical antipsychotic. What is it’s main side effect? Carbamazepine is another anti-convulsant with the same side effect.

A

Agranulocytosis (CBC done regularly)

38
Q

What kind of drug is citalopram

A

SSRI: sexual dysfunction is only big side effect

39
Q

Mechanism of action for the inotropic drug digoxin?

A

Inhibits NA-K-ATPase, which causes increase Na+ in cell, which causes increased Ca2+ and thus a stronger contraction.

40
Q

Urinary retention is common in postoperative hernia surgery. What drug can be given to help with this?

A

Muscarinic agonist (bethanechol) can be used, or an alpha 1 blocking drug.

This problem with incomplete bladder emptying is thought to involve decreased micturition reflex, decreased contractility of the bladder detrusor, and/or increased vesical sphincter tone.

Contraction of detrusor muscle is stimulated by muscarinic cholinergic agonists, like bethanechol)

41
Q

What do we use finasteride for?

A

5-alpha reductase inhibitor used to treat patients (men) with bladder outlet obstruction secondary to benign prostatic hypertrophy. This drug decreases conversion of testosterone to dihydrotestosterone in the prostate (so it shrinks). The latter is what causes the hypertrophy.

42
Q

What kind of effect does the drug phenyleprine have on the bladder?

A

It is an alpha-agonist with some selectivity for alpha 1 receptors, which causes contraction of the bladder sphincter muscle, so it would increase urinary retention.

43
Q

What happens when when you use an antidepressant in the depressive phase of bipolar disorder (like a TCA like imipramine)?

A

It can precipitate mania.

44
Q

How do proton pump inhibitors block gastric acid secretion?

A

Acts at the parietal cell apical membrane H+/K+-ATPase proton pump, which the final common pathway for HCl secretion. Lansoprazole is an example of this type of drug.

The final common pathway of gastric acid secretion from parietal cells is stimulated by ACh, histamine and gastrin.

45
Q

A drug that treats acute angle-closure glaucoma, which is also a diuretic works on what enzyme?

A

Carbonic anhydrase.

46
Q

The antidiabetic drug metformin is contraindicated with people with RENAL FAILURE, as well as liver dysfunction, CHF, alcoholism and sepsis. Why?

A

Metformin can cause lactic acidosis.

47
Q

Which of the drugs cause hypokalemia?
Which cause hyperkalemia?

Loop diuretics
spironolactone
Ace inhibitors
Angiotensin recpetor blockers

A

Loop: hypokalemia

All of the others can cause hyperkalemia

48
Q

Thiazolininediones are type II diabetic drugs that exert their glucose-lowering effect by improving insulin resistance.

  1. What is their mechanism of action?
  2. What is the most common side effect?

Example of thiozolidinediones is PIOGLITAZONE.

A
  1. Bind to peroxisome proliferator activated receptor gamma (PPAR-gamma) and activated it.
  2. Fluid retention which results in weight gain and edema Note: this excess fluid can exacerbate underlying CHF.
49
Q

Benzos are sedative hypnotic drugs with anxiolytic, muscle relaxant and anticonvulsant actions. They bind and modulate the GABA A receptor- _____________ channel in CNS neurons, increasing its frequently of opening.

A

Chloride

The hyper polarization will stabilize the membrane, rendering it less excitable.

50
Q

What is the mechanism of action for barbituates?

A

increase the during of opening of the GABAa receptor-chloride channel in CNS neurons. They bind to different site than benzos (which increase FREQUENCY of the opening of the channel), they have similar effects. But barbituates have a much longer half life, so you would not give them for insomnia.

51
Q

Serotonin syndrome is characterized by confusion, agitation, tremor, tachycardia, hypertension, clonus, hyperreflexia, hyperthermia and diaphoresis. Any drug that increases serotonin levels can cause this. What amino acid is a precursor for serotonin?

A

Tryptophan

52
Q

Glutamic acid is precursor for what neurotransmitter?
Histadine is precursor for?
Tyrosine?

A
  1. Glutamic acid–>GABA (inhibitory neurotransmitter)
  2. Histadine: histamine (atopic allergic reactions)
  3. Tyrosine: thyroxine, dopamine, epi and norepi
53
Q

Serotonin syndrome is most often seen when an SSRI is given with

A

MOA-I

54
Q

What is the drug cyproheptadine used for?

A

It is an antihistamine but it can be used to treat serotonin syndrome as it also has antiserotoneric properties.

Serotonin syndrome: characterized by mental status changes, neuromuscular dysfunction, autonomic instability (rapid and large changes in blood pressure and heart rate)

55
Q

Carbamazepine is used to treat simple partial, complex partial and generalized tonic-clonic seizures. What is its mechanism of action?

What is a major side effect?

A

Mechanism of action: blocks voltage-gated Na+ channels in cortical neuron membranes.

Side effect: bone marrow suppression, so CBC often. It also is hepatotoxic, so LFTs should be monitored regularly.

Note: A carbamazepin-associated increase in ADH secretion may cause SIADH.

56
Q

Ethosuximide blocks T-type Ca2+ channels and decreases calcium current in thalamic neurons. What is it the treatment of choice for?

A

Anticonvulsant that is the agent of choice for absence seizures.

57
Q

When a patient experiences drug-induced parkinsonism while being treated for psychosis, why can you NOT give levadopa to this person?

A

It can PRECIPITATE PSYCHOSIS!!!

58
Q

What kind of drugs are preferred with medication-induced parkinsonism?

A

Antimuscarinic agents (trihexyphenidyl and BENZTROPINE)…these are anticholinergics.

59
Q

Mechanism of action of methimazole.

A

inhibit thyroid peroxidase, which will prevent iodine organification and coupling of iodotyrosines.

Note: propylthiouracil does the same thing, but it ALSO blocks peripheral conversion of T4 to the more active form of T3.

60
Q

Sildenafil is a drug that is used to treat sexual dysfunction. What is the mechanism of action?

A

selective inhibitor of cGMP phosphodiesterase, which will prevent degradation of cGMP leading to higher intracellular levels. Nitric oxide and natruietic peptide both act via cGMP second messenger system (NO being primarily repsonsible for erection), and binding these hormones to their receptors will also increase intracellular cGMP concentrations.

61
Q

What receptor is responsible for contraction of uterus?

What receptor is responsible for eye dilation?

A

Uterus relaxation: beta 2

Pupil dilation: alpha 1