click below
click below
Normal Size Small Size show me how
Pharmacology
UWORLD Round 1
Question | Answer |
---|---|
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 |