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Pharmacology

UWORLD Round 1

QuestionAnswer
What is the main use for Flumazenil? Reversal agent for Benzodiazepine intoxication
What is used for reversing Benzodiazepine overdose? Flumazenil
What are the clinical symptoms of Benzodiazepine overdose? Somnolence, respiratory depression, amnesia, and ataxia
What is the mode of action of Flumazenil? Competitive antagonist of GABA-A receptor
What is the mode of action of Benzodiazepine? Facilitate GABA-A action by increased frequency of Chloride channel opening
Do benzodiazepines increase the frequency or duration of Cl- channel opening? Frequency
Which type of antiepileptics are know to facilitate GABA-A action by increasing the frequency of Cl- channel opening? Benzodiazepines
Which type of medication works by increasing the duration of Cl-channel opening order to facilitate the action of GABA-A receptors? Barbiturates
Common competitive antagonist of GABA receptor Flumazenil
What is "HIT"? Potentially fatal disorder characterized by extreme thrombocytopenia and an increased risk of thrombosis
Besides discontinuing Heparin, what medication is used to treat HIT? Argatroban
What is the mode action of Argatroban? Direct thrombin inhibitor
What type of medication is often used to treat HIT? Direct thrombin inhibitor
When is Protamine sulfate used in heparin adverse effects? Reverse the effects of Heparin in cases of an overdose with associated bleeding
What is the MOA of Heparin? Activates antithrombin, which decreased action primarily of factors IIa (thrombin) and Xa
What is activated directly by heparin? Antithrombin
Which medication is known to activate anti-thrombin? Heparin
What factors' action is decreased by Heparin? IIa (thrombin) and Xa
What are the most common adverse effects associated with Protease inhibitors? GI intolerance and Lipodystrophy
What kind of HIV medication is known to cause Lipodystrophy as an adverse effect? Protease inhibitors
What is the common ending of the nomenclature of Protease inhibitors? -navir
What kind of HIV medication usually ends in "-navir"? Protease inhibitors
Which antimycotic drug is contraindicated to be co-administered with Protease inhibitors? Rifampin
Common and potent CYP/UGT that is avoided or contraindicated in use with Protease inhibitors? Rifampin
Protease inhibitors can be used Rifampin or Rifabutin? Rifabutin
Which are Protease inhibitors not used with Rifampin? Reduces protease inhibitor concentration, as Rifampin isn a potent CYP/UGT inducer
What type of drug is Raltegravir? Integrase inhibitor
What is the common adverse effect associated with Integrase inhibitors? Increased creatine kinase
If a (+) HIV patient has increased serum level for creatine kinase, it is safe to assume part of the HAART is what type of medication? Integrase inhibitors
What is the key or common nomenclature feature of all Integrase inhibitors? -tegra-
What is the suffix in Integrase inhibitors? -gravir
What are the two most severe adverse effects of Lamotrigine? 1. Steven Johnson Syndrome 2. Hemophagocytic Lymphohistiocytosis
What is the "black box warning" of Lamotrigine? Hemophagocytic Lymphohistiocytosis
What is the mode of action Lamotrigine? Blockage of voltage-gated sodium (Na+) channels inhibit release of glutamate
Which antiepileptic is often associated with skin rashes of different severity? Lamotrigine
Common antiepileptic that works by blocking voltage-gated Na+ channels, inhibiting release of glutamate Lamotrigine
What causes HIT? Development of antibodies against Heparin-bound platelet factor 4
What is the pathological consequence of antibodies against Heparin-bound platelet factor 4? Clot formation
Which condition is often treated with Direct Thrombin inhibitors? HIT
Common Thiazolidinedione Pioglitazone
Which glucose lowering medications are known as the "glits"? Thiazolidinediones
What it the MOA of Thiazolidinediones? Act on Peroxisome Proliferator-Activating Receptor (PPAR) to sensitize skeletal muscle and liver to insulin
What is the most important adverse effect of Thiazolidinediones? Water retention
What type of diabetic medication is often associated with possible exacerbation or development of heart failure? Thiazolidinediones
Do CYP450 inducers or inhibitors increase metabolism of substrates (warfarin)? Inducers
What are the results or consequences of co-administering CYP450 inducers and Warfarin? 1. Inadequate anticoagulation 2. Decreased INR
What is the expected INR range of a patient with anticoagulation therapy after surgery? 2.5-3.5
List of the most common CYP450 system Inducers: 1. Chronic alcohol use 2. St. John's wort 3. Phenytoin 4. Phenobarbital 5. Griseofulvin 6. Nevirapine 7. Modafinil 8. Carbamazepine 9. Rifampin
List of common CYP450 system Inhibitors: 1. Sodium valproate 2. Isoniazid 3. Cimetidine 4. Ketoconazole 5. Acute alcohol overuse 6. Chloramphenicol 7. Erythromycin/ Clarithromycin 8. Omeprazole 9. Metronidazole 10. Amiodarone 11. Ritonavir 12. Grapefruit juice
What are common CYP450 system substrates? Warfarin, OCPs, Theophylline, and Antiepileptics
CYP-450 system INDUCER or INHIBITOR? Chronic alcohol use Inducer
CYP-450 system INDUCER or INHIBITOR? St. John's wort Inducer
CYP-450 system INDUCER or INHIBITOR? Phenytoin Inducer
CYP-450 system INDUCER or INHIBITOR? Phenobarbital Inducer
CYP-450 system INDUCER or INHIBITOR? Griseofulvin Inducer
CYP-450 system INDUCER or INHIBITOR? Nevirapine Inducer
CYP-450 system INDUCER or INHIBITOR? Modafinil Inducer
CYP-450 system INDUCER or INHIBITOR? Carbamazepine Inducer
CYP-450 system INDUCER or INHIBITOR? Rifampin Inducer
CYP-450 system INDUCER or INHIBITOR? Valproate Inhibitor
CYP-450 system INDUCER or INHIBITOR? Isoniazid Inhibitor
CYP-450 system INDUCER or INHIBITOR? Cimetidine Inhibitor
CYP-450 system INDUCER or INHIBITOR? Ketoconazole Inhibitor
CYP-450 system INDUCER or INHIBITOR? Acute alcohol abuse Inhibitor
CYP-450 system INDUCER or INHIBITOR? Chloramphenicol Inhibitor
CYP-450 system INDUCER or INHIBITOR? Sulfonamides Inhibitor
CYP-450 system INDUCER or INHIBITOR? Ciprofloxacin Inhibitor
CYP-450 system INDUCER or INHIBITOR? Omeprazole Inhibitor
CYP-450 system INDUCER or INHIBITOR? Metronidazole Inhibitor
CYP-450 system INDUCER or INHIBITOR? Amiodarone Inhibitor
CYP-450 system INDUCER or INHIBITOR? Ritonavir Inhibitor
CYP-450 system INDUCER or INHIBITOR? Grapefruit juice Inhibitor
CYP-450 system INDUCER or INHIBITOR? Erythromycin and Clarithromycin Inhibitor
Are atypical antipsychotics first or second generation? Second generation
What are adverse effects closely associated with Olanzapine and Clozapine? Hyperglycemia, Diabetes mellitus, and acute onset of DKA
How is adverse effects due to Olanzapine and Clozapine immediately treated? Discontinue medication
What are two common Atypical antipsychotics associated with DM, DKA, and hyperglycemia? Olanzapine and Clozapine
What is the MOA of Macrolide? Inhibit protein synthesis by blocking translocation
How do Macrolides prevent translocation? Binding to 23S rRNA of the 50S ribosomal subunit
What antibiotic category binds to the 23S rRNA of the 50S ribosomal subunit? Macrolides
What is the 1st line of treatment (antibiotic) for S. pyogenes causing Streptococcal pharyngitis? Penicillins
In a patient with Streptococcal pharyngitis with a strong penicillin allergy, it is instead treated which what antibiotic tpe? Macrolides
What are the symptoms of Strep pharyngitis? Fatigue, sore throat, fever, and tender anterior cervical lymphadenopathy
Which lymph area is affected most often in Strep pharyngitis? Anterior Cervical lymphadenopathy
List of adverse effects associated with Lithium: 1. Hypothyroidism (TH gland) 2. Ebstein anomaly (heart) 3. Nephrogenic Diabetes Insipidus (kidney) 4. Tremors
What is the associated renal side effect of chronic use of Lithium? Nephrogenic Diabetes insipidus
Does Lithium cause nephrogenic or central DI? Nephrogenic Diabetes insipidus
What is the cardiac anomaly associated with Lithium? Ebstein anomaly
Is Lithium toxicity or adverse effects associated with hypo- or hyperthyroidism? Hypothyroidism
Which two types of antidepressants work by preventing presynaptic reuptake of NE and Serotonin in noraderneige cell? Tricyclic antidepressants and SNRI
What is the mode of action of TCAs and SNRIs? Prevent (block) reuptake of NE and Serotonin in the Noradrenergic cell
Which organ is associated with the Organic Anion Transporter (OAT)? Kidneys
What is an important mediation used to prevent Gout? Probenecid
How does Probenecid prevent gout? Inhibiting the OAT in the kidneys
What is the main role of OAT? Important in the elimination of drugs in the kidneys
Why is Penicillin and other drugs' dosages lower when they are used concurrently with Probenecid? Probenecid inhibits OAT in kidneys, thus decreasing the clearance of those other drugs
What is a common and severe infection of the female reproductive organs caused by C. trachomatis and/or N. gonorrhoeae? PID
What is the best treatment duo (combination) for PID? Ceftriaxone and Doxycycline
What female reproductive infection is often treated with both, Ceftriaxone and Doxycycline? PID
Flumazenil if combined with a Barbiturate will: Have no effect since it only works to reverse Benzodiazepine overdose
What is the mode of action of Barbiturates? Increasing the duration of Cl- channel opening, thereby increasing the activity of the GABA-A receptor to induce sedation
What are common depressions caused by Barbiturate use? Cardiovascular, respiratory, and CNS
Does Barbiturates increase the Cl- channel opening duration or frequency? Duration
What is the most common tested (USMLE) Thiazide? HCTZ
What type of diuretic is HCTZ? Thiazide diuretic
What is MOA of HCTZ? Inhibits the reabsorb of NaCl in the DCT and decreases calcium excretion
How is calcium (Ca2+) affected by Thiazide diuretics? Decreases excretion of Ca2+
Where in the nephron does HCTZ work? Distal convoluted tubule
What is the most common thiazide used to treat Hypertension? HCTZ
What precipitates acute pancreatitis in patient on HCTZ? It decreases Ca2+ excretion, leading to Hypercalcemia which may precipitate acute pancreatitis
What adverse effect of Thiazide diuretics cause acute pancreatitis? Decreased Calcium excretion causing hypercalcemia
Beta-lactam antibiotic that block cell synthesis by inhibiting peptidoglycan cross-linking. Penicillins
What is the 1st line of treatment of Streptococcal pharyngitis? Penicillins
MOA of Penicillins Block cell wall synthesis by inhibiting peptidoglycan cross-linking; B-lactam antibiotic
Why are 1st and 2nd generation cephalosporins used to prevent surgical infections prior to surgery? Excellent activity against gram (+) bacteria
What is the most common cause of post-surgical infections? Gram (+) bacteria infections
What is the most common diuretic used to treat hyperkalemia? Furosemide
What type of diuretic is Furosemide? Loop diuretic
What is a serious adverse effect of Clozapine (exclusively)? Agranulocytosis
Which atypical antipsychotic is often associated with Agranulocytosis? Clozapine
What is the most common use for Clozapine? Refractive schizophrenia
Which are drugs have shown to improve long-term survival in patients with heart failure due to left ventricular systolic dysfunction? B-blockers, ACE inhibitors, ARBs, and aldosterone antagonists
What is Milrinone? A phosphodiesterase-3 inhibitor
What specific enzyme is inhibited by Milrinone? Phosphodiesterase-3
What is the benefit to cardiomyocytes by Milrinone? Calcium influx into cardiomyocytes is increased, which increases cardiac contractility
How does Milrinone increase cardiac contractility? Increasing calcium influx into cardiomyocytes as Phosphodiesterase-3 is inhibited
What is the effect on cardiovascular smooth muscle done by Milrinone? Calcium-Myosin light chain kinase interaction is reduced, which causes vasodilation and reduces cardiac preload and afterload
Are Preload and Afterload increased, reduced, or stay normal with the use of Milrinone? Both are reduced
Which enzyme interactions recued or partially inhibited by Milrinone that leads to vasodilation and a decreased preload & afterload? Calcium-Myosin light chain kinase
What enzymes are inhibited by Milrinone? Phosphodiesterase-3 and Calcium-Myosin light chain kinase
What is the function of Phosphodiesterase-3 inhibitor? Reduction of the degradation of cyclic adenosine monophosphate (cAMP) to provide two beneficial effects to treat systolic heart failure
Milirinoe is more commonly used to treat systolic or diastolic heart failure? Systolic heart failure
The use of Milrinone increases or decreases amount of cAMP? Increases cAMP concentration
What therapy is usually used in patients with an acute ST segment elevation MI? Fibrinolytic therapy as reasonable REPERFUSION technique in patients with no contraindication to thrombolysis
How do common fibrinolytics work? Bind to fibrin in the thrombus (clot) and activate plasmin, which leads to thrombolysis
What is the most common adverse effect of Fibrinolytic therapy? GI and/or Intracerebral hemorrhage
Which patients are usually contraindicated to receive Fibrinolytic therapy? Those with contraindications to thrombolysis
What is a common Fibrinolytic agent? Alteplase
What is Phenoxybenzamine? An irreversibly a-1 and a-2 adrenergic antagonist that effectively reduces the arterial vasoconstriction induced by norepinephrine
Why are effects of Phenoxybenzamine not overcome with increasing concentration of norepinephrine? Phenoxybenzamine is an irrevocably alpha-1 and alpha -2 antagonist
What are two common Class III antiarrhythmics? Dofetilide and Ibutilide
What class of antiarrhythmic is Dofetilide? Class III
What common atrial arrhythmia is often treated with a Class III antiarrhythmic, such as Dofetilide? Atrial Fibrillation
What channel is blocked or affected by Class III antiarrhythmics? K+ channel
What are the effects on the AP by using Dofetilide and other Class III antiarrhythmics? Slow down repolarization and increase the effective refractory period
How is the Effective refractory period affected by Class III antiarrhythmics? Increased
What is the effect on ECG tracings by Class III antiarrhythmics? QT interval is prolonged, creating an increased risk of polymorphic ventricular arrhythmias
What is a common arrhythmia caused by the side effects of class III antiarrhythmics? Torsades de Pointes
What kind of arrhythmia is Torsades de Pointes? Polymorphic ventricular tachycardia
What is the change in 2nd messenger with stimulation of alpha-1 receptors? Increase IP3
Which sympathomimetic receptors increase IP3 (second messenger) activity as they are stimulated? Alpha-1 and Muscarinic-3
Is cAMP activity increased or decreased by stimulation of B-1 and B-2 receptors? Increased
What is the change in second messenger activity as alpha-2 rectprost are stimulated? Descrased in cAMP activity
If cAMP (2nd messenger) activity is decreased, which are common sympathomimetic receptors that are likely stimulated? Alpha-2 and Muscarinic-2
What are the primary effects of alpha-1 stimulation? 1. Peripheral vasoconstriction 2. Urethral contraction 3. Pupillary dilation
Does the stimulation of alpha-1 receptors cause pupillary dilation or pupillary contraction? Pupillary dilation
What are two primary effects caused by alpha-2 receptor stimulation? 1. CNS sympatholytic 2. Decreased insulin release and intestinal motility
How is the nephron involved in the pathogenesis of diabetic nephropathy? Excess glucose in PCT causes increased reabsorption of sodium by Sodium-Glucose Cotransporter 2 (SGLT-2)
What is the result of excess glucose causing PCT to reabsorb sodium through the SGLT-2, leading to Diabetic nephropathy? Decrease delivery of sodium to the macula densa and increased secretion of Renin, ultimately hyperfiltration
What important renal-release enzyme is secreted in excess in Diabetic nephropathy? Renin
What is the function of SGLT-2 inhibitors? Increase the delivery of sodium to the macula densa, decreasing renin production and reducing hyperfiltration
What diabetic medication category works by increasing the delivery of Sodium to the Macula densa? SGLT-2 inhibitors
What are the results of SGLT-2 inhibitors delivering increased amounts of Na+ to the Macula densa? 1. Decrease Renin production by JG cells 2. Reducing hyperfiltration
What are the products of proinsulin as it is cleaved? Insulin and C-peptide in equimolar quantities
What does levels of C-peptide in blood indicate? Endogenous insulin secretion
High levels of circulating C-peptide, would indicate? Elevated secretion of endogenous insulin
Which diabetic type of medication would produce an elevated C-peptide level? Sulfonylureas and Meglitinides
How do Sulfonylureas and Meglitinides help diabetic patients? Lower blood glucose by stimulating pancreas insulin production; the hypoglycemia produced by these is associated with elevated C-peptide
What is the main contraindication for OCP use? Prior Hx of thromboembolic events or strokes
List of Contraindication for OCP therapy? 1. Hx of prior thromboembolic events or strokes 2. Hx of estrogen-dependent tumor 3. Women > 35 years old who smoke heavily 4. Hypertriglyceridemia 5. Decompensated or active liver disease 6. Pregnancy
What are two common stimulant laxatives? Bisacodyl and Senna
What condition is treated with Bisacodyl? Stimulant laxative
What is the mode of action of Bisacodyl? Stimulant laxative that stimulates the enteric neurons writing the colonic myenteric plexus, thereby increases peristaltic activity and enhancing colonic motility
What part of the nervous system is stimulated by Bisacodyl? Enteric neurons within the colonic myenteric plexus
What are associated adverse effects of Stimulant laxatives, such as Senna and Bisacodyl? Abdominal cramping and electrolyte disturbances
Common folic acid antagonist Methotrexate
What is a non-neoplastic condition treated with MTX? Ectopic pregnancy
What enzyme is inhibited by MTX? DHF reductase
What is the role of DHF reductase? Catalyze the synthesis of Tetrahydrofolate
What does the inhibition of DHF reductase by MTX cause accumulation of? Dihydrofolate polyglutamate
What condition or event would cause the intracellular accumulation of Dihydrofolate polyglutamate? MTX inhibition of DHF reductase
What two types of antibiotics are often associated with development of drug-induced hemolytic anemia? Penicillins and Cephalosporins
How can Penicillins and Cephalosporin cause hemolytic anemia? As they can bind to erythrocyte surface and act as HAPTENS for IgG attachment, which lead to splenic macrophages lead to hemolytic anemia
What hematologic condition is associated as penicillins act as Haptens? Penicillin (drug)-induced hemolytic anemia
What does arteriovenous concentration gradient reflect on anesthesia? Tissue solubility of an anesthetic
A anesthetic with a high tissue solubility will have: 1. Large arteriovenous concentration gradient 2. Slow onset of action
Is the onset of action of a anesthetic with high tissue solubility is fast or slow? Slow onset of action
Large arteriovenous concentration gradient means what to anesthetic solubility? High tissue solubility of the anesthetic
What are Transient Ischemic Attacks (TIA)? Transient episode of focal neurologic impairment that occur due to local brain ischemia
Is there tissue infarction with TIAs? No; tissue infarction does not occur and brain imaging is normal
What is a risk to develop in patients with TIA? Stroke
How is a stroke prevented in patients with TIA? Antiplatelet agents (aspirin, clopidogrel), statins, and lifestyle modifications (tobacco cessation, exercise)
What are two very common antiplatelet agents? Aspirin and Clopidogrel
What is P-glycoprotein? Efflux pump found on the brain capillary endothelial cells (part of the BBB) that inhibits a wide range of substrates from entering the brain
Does p-glycoprotein act to facilitate or prevent entrance of substrates into the brain? Prevent entrance
What does the inhibition of P-glycoprotein cause? Improve drug delivery to the CNS
What would be a way to deliver higher amounts of a drug ht is normally impermeable to the BBB? By inhibition of ht eh p-glycoprotein
What receptors are blocked by atypical (2nd gen) antipsychotics? Dopamine D2 receptors and Serotonin 2A receptors
Which drugs are known to have antagonism to the dopamine D2 and 5-HT2A receptors? Atypical antipsychotics
What are some associated adverse effects of atypical antipsychotics? Metabolic syndrome, weight gain, and ESP (although less common than typical antipsychotics)
Extrapyramidal symptoms due to adverse reaction to antipsychotics are more common in 1st or 2nd generation antipsychotics? 1st generation (typical) antipsychotics
What is Empyema? Bacterial invasion of the intrapleural space with progressive inflammation, pus accumulation and organized fibrosis
Bacterial infection of the intrapleural space leading to pus and fibrosis. Empyema
What actions can help drainage of effusion through the chest tube? Administration of fibrinolytic agent (tPA) in combination with a nucleic acid cleaving enzyme (deoxyribonuclease)
What makes difficult the drainage of an empyema through a chest tube? Location of tube and effusion, as well the high viscosity of the effusion
What is a commonly used Vaptan? Tolvaptan
What are the Vaptans? Vasopressin V2 receptor antagonists
What electrolyte imbalance is often treated with Vaptan? Hyponatremia
Which vasopressin receptor is targeted by Vaptans? Vasopressin V2 receptors
How do Vaptan treat hyponatremia? Vaptans block the effects of ADH, increasing free water excretion without directly affecting excretion of Na+ and K+
What type of medication are known to block the effects of ADH, increase free water excretion while not affecting Na+ and K+ excretion? Vaptan
What are the results of the diuresis of free water with Vaptan use? 1. Increased plasma osmolality 2. Increased serum sodium 3. Increased urine output 4. Lowered urine osmolality
What does "low serum osmolality" mean? Low amount of dissolved particles in the blood
A high osmolality, refers to urine or blood with a high or low concentration? High concentration as many particles are dissolved
What is the effect on blood pressure caused by alpha-adrenergic agonists? Increased systolic and diastolic blood pressure
Created by: rakomi
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