HIV drugs and antibiotics that can't be used in pregnancy

Question 1

typical HAART therapy

Answer 1

give 2 nucleoside reverse transcriptase inhibitors and one non-nucleoside reverse transcriptase inhibitor or 1 protease inhibitor or 1 integrase inhibitor

Question 2

protease inhibitors: drug name, mechanism

Answer 2

all of these drugs end in -navir.
recall that virion assembly requires HIV-1 protease, which cleaves the products of HIV mRNA into functional parts. protease inhibitors prevent the maturation of new viruses.

Question 3

ritonavir considerations

Answer 3

this is a protease inhibitor that can boost other drug concentrations by inhibition cytochrome P-450.

Question 4

toxicity of protease inhibitors

Answer 4

hyperglycemia, GI intolerance, lipodystrophy. indinavir can cause nephropathy and hematuria

Question 5

NRTIs. Exceptions within this group?

Answer 5

nucleoside reverse transcriptase inhibitors. these all inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (they lack a 3’ OH group). tenofovir is a nucleotide, all others are nucleosides that must be phosphorylated to be active.

Question 6

What drug is used to decrease the likelihood of fetal transmission during pregnancy?

Answer 6

ZDV (zidovudine, used to be called AZT)

Question 7

toxicity of the NRTIs

Answer 7

bone marrow suppression (may be reversed with G-CSF and erythropoietin), peripheral neuropathy, lactic acidosis (except tenofovir), rash, anemia (ZDV), pancreatitis (esp. didanosine)

Question 8

Efavirenz

Answer 8

this is an NNRTI (non-nucleoside reverse transcriptase inhibitor). others include nevirapine, and delaviridine. these bind to RT at a side different from NRTIs. they don’t require phosphorylation to be active or compete with nucleotides.

Question 9

NNRTI toxicities

Answer 9

all case rash and hepatotoxicity. vivid dreams and CNS symptoms are seen with efavirenz. delaviridine and efavirenze are contraindicated in pregnancy

Question 10

integrase inhibitor

Answer 10

raltegravir. this inhibits HIV genome integration into the hose cell by reversibly inhibiting HIV integrase.

Question 11

raltegravir toxicity

Answer 11

hypercholesterolemia

Question 12

enfuvirtide: mechanism

Answer 12

binds gp41 to inhibit viral entry and can cause skin rxn at injection site

Question 13

maraviroc mechanism

Answer 13

binds CCR-5 on surface T cells/monocytes to inhibit interaction with gp120.

Question 14

interferon mechanism

Answer 14

these are glycoproteins usually made by virus infected cells. they exhibit many antiviral and antitumor properites

Question 15

IFN-alpha

Answer 15

used for chronic hep B and C, kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcionoma, and malignant myeloma.

Question 16

IFN-beta

Answer 16

used in multiple sclerosis

Question 17

IFN-gamma

Answer 17

used in chronic granulomatous disease

Question 18

toxicities of interferons

Answer 18

neutropenia and myopathy

Question 19

what antibiotics should be avoided in pregnancy?

Answer 19

sulfonamides (kernicteris) aminoglycosides (ototoxic), fluoroquinolones (cartilage damage), clarithromycin (embryotoxic), tetracyclines (discolored teeth and inhibition of bone growth), ribavirin (teratogenic), griseofulvan (teratogenic), chlormphenicol (grey baby syndrome) (SAFe Children Take Really Good Care)