S47(4) NNRTI's and PI's

Question 1

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Answer 1

Causes a conformational change of the reverse transcriptase

Question 2

doravirine (Pifeltro)

Place in therapy:

Answer 2

only recommended in certain situations

Question 3

efavirenz (Sustiva)

Place in therapy:

Answer 3

only recommended in certain situations

Question 4

efavirenz (Sustiva)

Counseling:

Answer 4

Take at bedtime on an empty stomach

High fat/calorie meals increase absorption and enhance likelihood of CNS effects

CNS: nightmares, trouble sleeping, delusions, anxiety, depression, psychosis, and more

TAKING AT NIGHT can help with NIGHTMARES and trouble sleeping

Question 5

efavirenz (Sustiva)

Other notes:

Answer 5

Do not use if HIV viral load > 100,000 copies

Question 6

rilpivirine (Edurant)

Place in therapy:

Answer 6

only recommended in certain situations

Question 7

rilpivirine (Edurant)

counseling:

Answer 7

Take whole with water and a normal to high calorie meal to increase absorption

DRUG – DRUG INTERACTIONS

CONTRAINDICATION WITH PPIs, use with caution with H2RAs or antacids

Question 8

rilpivirine (Edurant)

other notes:

Answer 8

DRUG – DRUG INTERACTIONS including warfarin and dexamethasone
Small tablet size

Do not use if viral load > 100,000 copies and/or CD4 < 200

Question 9

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Answer 9

doravirine (Pifeltro)
efavirenz (Sustiva)
rilpivirine (Edurant)

Question 10

Protease Inhibitors (PIs)
MOA:

Answer 10

Inhibit maturation of viral proteins needed to make a virion

Higher barrier to resistance

Question 11

Protease Inhibitors (PIs)
Class effects:

Answer 11

DRUG – DRUG INTERACTIONS

Metabolic changes
Hyperlipidemia
Lipodystophy/ fat redistribution (HUMP BACK)
Insulin resistance

GI distress

Question 12

Protease Inhibitors (PIs)

Answer 12

darunavir (Prezista)

ritonavir (Norvir)

Question 13

darunavir (Prezista)

Place in therapy:

Answer 13

only recommended in certain situations

Question 14

darunavir (Prezista)

Counseling:

Answer 14

Take with food to help with absorption and GI upset
DRUG – DRUG INTERACTIONS
MUST be boosted with PK enhancer
V/N/D, indigestion, abdominal pain

Question 15

darunavir (Prezista)

Other notes:

Answer 15

ALWAYS run a DDI check

MUST be boosted with PK enhancer

Question 16

darunavir (Prezista)

Pharmacokinetics (PK) Enhancers:

Answer 16

Ritonavir – PI that is used as boosting agent
ONLY used as a boosting agent
PIs MUST have a boosting agent

Cobicistat – not active against HIV, only used as a boosting agent