Pharmacology

Question 1

What class of drugs does Sacubitril belong to? Mechanism of action.

Answer 1

• Neprylisin inhibitor (ARNI - angiotensin receptor neprylisin inhibitor)→Tx heart failure (↓mortality, combined with ARB or alone)
• Nephrylisin→zinc-dependent metalloprotease►break bradykinin, natriuretic enzymes→↑bradykinin (relax cardiac muscle), ↑natriuretic peptides

Question 2

Why do you avoid prasugrel as a second anti-platelet drug for a patient with AMI undergoing to angioplasty and previous history of TIA or stroke?

Answer 2

Prasugrel has a higher incidence of intracranial incidence

Question 3

Treatment for hemolytic uremic syndrome.

Answer 3

Eculizumab→inhibit cleavage of C5►C5a/b→block complex formation that cause the hemolysis►prevent hemolysis

*Previously used for Paroxysmal nocturnal hemoglobinuria

Question 4

Mechanism of action of Ustekinumab? and indications.

Answer 4

• Biologic therapy targeting IL-12/IL-23

- Chron’s disease, primary billiary cirrhosis, Type 1 DM with residual beta islet cells, Psoriasis, psoriatic arthritis

Question 5

Which antibiotics have time-dependent bactericidal effect?

Answer 5

Cell-wall inhibitors like Beta-lactam→long time to exert their effect as cell wall building is slow

*Higher concentrations→NOT greater kill of organisms

Question 6

Indication of Reslizumab. Which other drug with the same mechanism of action exist?

Answer 6

• Add-on maintenance treatment for severe eosinophilic asthma no responsive to other medications
• Mepolizumab→IL-5 antagonist (same indication)

Question 7

Neuromuscular blocker of election for chronic kidney disease stage 5 and child-pugh C liver disease and why?

Answer 7

• Atracurium and Cisatracurium→undergo Hoffman degradation►change a quaternary amine to tertiary amine→ideal for renal and liver disease

Question 8

Mechanism of action and indication of Elbasvir/grazoprevir. Indications.

Answer 8

• Elbasvir→NS5A polymerase inhibitor
• Grazoprevir→NS3/4 protease inhibitor
• HCV genotype 1 and 4

Question 9

What condition you should rule out before begin Elbasvir/grazoprevir therapy in HCV type 1a and why?

Answer 9

• NS5A resistance associated variants
• HCV type 1a genotype→can be resistant to Elbasvir component at baseline before begin Tx
• If no resistance→Tx during 12 weeks
• If resistance→Tx during 16 weeks AND Ribavirin

Question 10

Monoclonal antibody approved for treatment of Gastric cancer and why?

Answer 10

• Trastuzumab→HER2 inhibitor
• HER2 is over-expressed in 10-25% of gastric cancers→tyrosine kinase receptor►affects proliferation, apoptosis, adhesion, migration, differentiation
• Lower mortality rate in gastric cancer (usually with cisplatin or 5-flurouracil)

*Very used for breast cancer

Question 11

Common toxicity presentation of phenytoin

Answer 11

Confusion, dysarthria, diplopia, VERTICAL nystagmus (one of the fewer causes of it)

Question 12

Perampanel

Answer 12

• AMPA (amino methyl isoxazolepropionic acid) receptor antagonist [Glutamate receptor]
• Seizures

Question 13

Peramivir (IV administration). Other drugs of its class.

Answer 13

• Neuraminidase inhibitor→Oseltamivir (oral), Zanamivir (inhalation)
• Influenza A and B virus

Question 14

Colbicistat

Answer 14

• CYP3A4 inhibitor→pharmacokinetic enhancer of other antiviral drugs

Question 15

Benzodiazepine that is not metabolized by CYP450

Answer 15

Lorazepam

*Does not interact with CYP450 inhibitors

Question 16

Pre-exposure (PrEP) and post-exposure prophylaxis (PEP) for HIV

Answer 16

• PrEP→Risk patients (men who have sex with men, IV drug users, who DON’T have infection)►Tenofovir/Emtricitabine
• PEP→Ex, healthcare professional suffer needle stick injury►Tenofovir/Emtricitabine (once day) + Raltefravir (twice day) by 28 days [best take within 72 hrs after exposure)

Question 17

Treatment of infantile hemangioma

Answer 17

• Infantile hemangioma→Beta-adrenergic receptor mediated vascular dysfunction►↑proliferation and angiogenesis
• Propranolol (oral solution), Timolol (topically)→↓pro-angiogenic factors►VEGF, B-FGF