Analgesics

Question 1

Anti-migraine medications (4)

Answer 1

• Perfenazine
• Rizatriptan
• Natalizumab
• Zolmitripan

Question 2

Triptan (riza or zolmi) mechanism of action

Answer 2

Selective serotonin agonists —> 5-HT1b/1d
- Vasoconstriction
- Inhibit trigeminal nerve nociception
- Inhibit vasoactive peptide secretion

Question 3

Triptan side effects

Answer 3

• Paresthesia, cold sensation
• Serotonin sx
• Hypertension
• Vasospasm = ischemia

Question 4

When should triptans NOT be given?

Answer 4

Within 24 hrs of ergot derivate, another 5HT agonist or SSRIs —> coronary spasm of serotonin sx

History of coronary artery disease or hypertension

Question 5

Triptan ADME

Answer 5

A: oral, SC, nasal
D: low bound to proteins, cross placenta
M: riza = MAO; zolmi = CYP1A2 and MAO
E: urine

Question 6

Perphenazine mechanism of action

Answer 6

D2 antagonist
—> antipsychotic 1st gen
—> extrapyramidal effects, strong antiemetic

Question 7

Perphenazine main uses (3)

Answer 7

• Schizophrenia
• Acute anxiety
• Severe nausea and vomiting

Question 8

Perphenazine side effects (6)

Answer 8

• Extrapyramidal
• Neuroleptic malignant sx = more reflex, rigidity
• Hyperprolactinemia
• Hypotensino
• Weight gain
• CNS depression, seizures

Question 9

Perphenazine ADME

Answer 9

A: oral
D: protein bound, widely distributes, crosses placenta
M: CYP2D6
E: urine and feces

Question 10

Natalizumab mechanism of action

Answer 10

Target: a4 integrin
—> affects WBC adhesion and migration

Question 11

Natalizumab uses

Answer 11

• MS
• Crohn
• Migraine? (Según clasificación del Dr)

Question 12

Natalizumab main possible side effect

Answer 12

Reactivation of latent JC virus —> PML

Question 13

NSAID mechanism of action

Answer 13

Inhibition of COX1 and COX2 = less PGs
(Only irreversible is acetylsalicylic acid)

COX1: constitutively
COX2: mostly CNS

Question 14

COX2 selective inhibitor

Answer 14

Celecoxib

Question 15

NSAID ADME

Answer 15

A: rapid oral absorption
D: 95-99% protein bound, wide distribution
M: hepatic biotransformation
E: urine

Question 16

NSAID uses (5)

Answer 16

• Anti-inflammatory (RA)
• Analgesic
• Antipyretic
• Antiplatelet
• Uricosuric (gout)

Other: PDA closure, mastocytosis, niacin tolerance

Question 17

NSAID side effects

Answer 17

• GI: ulcers, reflux, pain, diarrhea
• Hepatotoxicity
• CV: COX2 inhibition = thrombosis risk
• Renal: hypotension, nephropathy
• Pregnancy: NOT in 3rd trimester
• NOT 1-3 days before surgery

Question 18

Paracetamol main side effect

Answer 18

Hepatotoxicity id >4g/day
—> give N-acetylcysteine

Question 19

Paracetamol ADME

Answer 19

A: oral, IV
D: all tissues except fat
M: CYP2E1 —> NAPQI (toxic metabolite inactivated by glutathione)
E: urine

Question 20

Which NSAIDS have a higher potency?

Answer 20

Keterolac
Diclofenac - can cause elevated transaminases

Question 21

Sulindaco relevance as an NSAID

Answer 21

Increased anti-inflammatory activity

Question 22

Diclofenac ADME

Answer 22

A: oral
D: SYNOVIAL FLUID, 99% protein bound
M: CYP2C
E: urine and feces

Question 23

Naproxen relevance as an NSAID

Answer 23

Increased half life (9-25 hours)
More potency
Safer for people with CV history

Question 24

Ketoprofen relevance as an NSAID

Answer 24

Small half life (1-3 hours)
—> Quicker effect
Stronger than ibuprofen and diclofenac

Question 25

Piroxicam and meloxicam type of medication and uses

Answer 25

Enolic acid - RA - Osteoarthritis - Acute pain and inflammation

Question 26

Medications with some selectivity for COX2

Answer 26

- Celecoxib - Diclofenac - Meloxicam

Question 27

Enolic acid vs NSAID main difference

Answer 27

Enolic acids have a very high half life: —> piroxicam = 50 hours —> meloxicam = 15-20 hours

Question 28

Medication to use in patients with GI risk and why

Answer 28

Celecoxib, there are mostly COX1 receptors in the gastric mucosa

Question 29

Do NOT give celecoxib to patients with:

Answer 29

High cardiovascular risk Sulfa allergy

Question 30

Colchicine mechanism of action

Answer 30

Binds to tubulin subunit —> inhibit microtubule polymerization —> inhibit phagocytosis of urate crystals, neutrophil activation, migration, and degranulation = ANTI-GOUT AGENT

Question 31

Colchicine main side effects (5)

Answer 31

- Narrow therapeutic window - GI symptoms - Myelosuppression - Rhabdomyolysis - Toxicity: renal, cardiac, CNS

Question 32

Allopurinol mechanism of action

Answer 32

XANTHINE OXIDASE INHIBITION —> xanthine is not degraded into uric acid = less uric acid

Question 33

What is the first line agent for reducing uric acid in plasma?

Answer 33

Allopurinol (Give colchicine before in gout treatment)

Question 34

When allopurinol is combined with ______, it causes bone marrow toxicity.

Answer 34

Azathioprine

Question 35

Allopurinol ADME

Answer 35

A: oral, IV D: no protein binding, water distribution M E: urine

Question 36

Methocarbamol mechanism of action

Answer 36

CNS depressant - Sedative - Skeletal muscle relaxation ACUTE relief

Question 37

Methocarbamol ADME

Answer 37

A: oral, IV, IM D: 50% protein bound M: hepatic E: urine

Question 38

What type of medication is acemetacin?

Answer 38

NSAID Used for osteoarthritis, RA, back pain, post-op pain

Question 39

Allopurinol

Answer 39

Uric acid decrease

Question 40

Colchicine

Answer 40

Prevent gout attacks

Question 41

Diclofenac

Answer 41

NSAID Stronger than others

Question 42

Ketoprofen

Answer 42

NSAID Moderate-severe pain

Question 43

Meloxicam

Answer 43

NSAID Very strong, high risk of clots RA, low GI and renal side effects

Question 44

Methocarbamol

Answer 44

Muscle relaxant

Question 45

Naproxen

Answer 45

NSAID Long duration, safe when heart risk

Question 46

Piroxicam

Answer 46

NSAID Better at reducing swollen joints

Question 47

Sulindac

Answer 47

NSAID

Question 48

Acemetacin

Answer 48

NSAID AR and muscular

Question 49

Celecoxib

Answer 49

NSAID Lower GI risk

Question 50

Paracetamol

Answer 50

Analgesic and anti-pyretic

Question 51

Perphenazine

Answer 51

Anti-psychotic Scizophrenia Severe nausea and vomiting

Question 52

Rizatriptan

Answer 52

5-HT receptor agonist Migraine

Question 53

Natalizumab

Answer 53

Mab vs a4 integrin No leukocyte adhesion (MS and Crohn)

Question 54

Zolmitriptan

Answer 54

5-HT receptor agonist 1B and 1D Acute migraine

Question 55

Rizatriptan vs zolmitriptan

Answer 55

R: first choice of treatment Z: first choice for short-term