Pharmacology

Question 0

Calcitonin

Answer 0

Mech: BONE: Binds to Osteoclast receptors–> Inhibits bone resorption–> Decreased blood Ca2+ and Phosphate. KIDNEY: decreases resorption.
Uses: Hypercalcemia, neoplasia, Paget disease, osteoporosis.
SE: Nausea, vomiting, tingling sensation, unpleasant taste.

Question 1

Bisphosphonates

Answer 1

Risedronate, Alendronate, Clodronate, Etidronate, Ibandronate, Pamidronate, Tiludronate, Zoledronate
Mech: Binds to Bone–> inhibits Osteoclast bone resorption. Also stimulates osteoblasts activity
Uses: Osteoporosis, Paget disease, Hypercalcemia, Bone cancer
SE: GI disturbance (dyspepsia), bone pain

Question 2

Teriparatide

Answer 2

Recombinant PTH (Forteo)
Mech: KIDNEY: Stimulates Ca2+ absorption in Renal DCT. BONE: Ca2+ release.
Uses: Osteoporosis.
SE: Nausea, HA, dizziness, hypercalcemia, leg cramps

Question 3

Selective Estrogen Receptor Modulators (SERMs)

Answer 3

Raloxifene, Tamoxifen
Mech: Activates ERs in bone/cardio. Antagonizes ERs in Mammary/Uterus tissue. Inhibit cytokines, recruit osteoclasts, block PTH.
Uses: Prevention of osteoporosis, Breast cancer.
SE: Hot flashes, flushing, Increased risk for DVT and Pulm. embolism.

Question 4

TNF-alpha Antagonists

Answer 4

Adalimumab, Certolizumab, Etanercept, Golimumab, Infliximab
Mech: Block inflamm. cytokine TNF-alpha
Uses: RA, psoriasis, psoriatic arthritis, ankylosing spondylosis
SE: Hypersensitivity, infection, risk of malignancy

Question 5

List Drugs to treat Bone disorders

Answer 5

1. Bisphosphonates
2. Calcitonin
3. Teriparatide
4. Selective Estrogen Receptors Modulators
5. TNF-alpha Antagonists

Question 6

Colchicine

Answer 6

Mech: Prevents neutrophil and leukocyte migration into joint by binding to tubulin–> depolymerize Microtubules–> disrupting migration and degranulation
Uses: Gout (Acute and prophylaxis)
SE: GI disturbance, severe diarrhea, GI hemorrhage, Hepatic toxicity

Question 7

Xanthine Oxidase Inhibitors

Answer 7

Allopurinol, Febuxostat
Mech: Reduced synthesis of uric acid.
Uses: Chronic gout. NOT acute (can make worse).
Allopurinol–> also used for prevention of Urate Nephrolithiasis and Tumor Lysis Syndrome
SE: BOTH: GI disturbance, liver dysfunction. Allopurinol: Allergic skin reactions

Question 8

Probenecid

Answer 8

Mech: Inhibits absorption of uric acid in PCT–> increasing excretion.
Uses: Chronic gout. MUST have adequate renal fcn. Be careful w/ Penicillins (will increase Penicillin levels)
SE: Dyspepsia and peptic ulcers, drug-induced nephritic syndrome

Question 9

List drugs used to Gout

Answer 9

1. Colchicine
2. Xanthin-Oxidase Inhibitors
3. Probenecid

Question 10

Corticosteroids

Answer 10

Mech: bind to cytosolic receptors–> alter gene expression–> Inhibition of inflamm. cytokine production. Relieve mucosal inflammation, bronchial reactivity, and increases airway caliber
Uses: Disease flare-ups, acute inflammation, asthma
SE: Short-term: insomnia, dyspepsia, increased appetite, anxiety/psychosis. Long-term: Cushing’s syndrome, obesity, diabetes, osteoporosis, immune suppression.

Question 11

Cyclophosphamide

Answer 11

Mech: Liver metabolizes–> Active Phosphoramide mustard–> cross-links DNA and inhibit T- and B-cell fcn.
Uses: SLE, RA, vasculitis, cancer
SE: Ovaria failure, infertility, bone marrow suppression, risk for malignancy

Question 12

List drugs used to treat Connective Tissue Disorders

Answer 12

1. Cortiocosteroids

2. Cyclophosphamide

Question 13

Opioids

Answer 13

Mech: Bind/Activate Opioid receptors–> inhibit AC–> Open K+ channels–> Hyperpolarize–> inhibits transmitter release. Inhibit NT release
Uses: Pain relief, cough suppression, diarrhea, Acute pulmonary edema, opioid addicts, drug overdose
SE: sedation, resp. depression, miosis, constipation

Question 14

Different uses of Opioids and Corresponding meds (Contraindications)

Answer 14

Cough Suppression: Dextromethorphan
Diarrhea: Loperamide, Diphenoxylate
Opioid addiction: Methadone
Opioid Overdose: Naloxone and Naltrexone

***Contraindicated: Supp. O2 is contraindicated in COPD pt that had Morphine overdose.

Question 15

Aspirin

Answer 15

Mech: Acetylates and IRREVERSIBLY inhbits COX-1 and COX-2–> prevent conversion of Arachidonic acid to PGs
Uses: Antipyretic, analgesic, anti-inflamm, anti-platelet activity, Kawasaki, OA, inflamm. arthritides
SE: Increase bleeding (NO effect on PT or PTT), Gastric ulcers, hyperventilation, Reye syndrome, tinnitus.

Question 16

Nonsteroidal Anti-Inflammatory Drugs

Answer 16

Ibuprofen, Naproxen, Indomethacin, Ketorolac, others
Mech: REVERSIBLY inhibits Arachidonic acid and COX-1/2–> inhibit production of PGs and Thromboxanes
Uses: Anti-inflammatory, analgesic, antipyretic, anti-platelet effects.
SE: Renal damage, aplastic anemia, GI distress, ulcers, fluid retention, HTN

Question 17

COX-1 vs. COX-2

Answer 17

COX-1: constitutive enzyme in most tissues, including platelets
COX-2: induced in inflammatory cells upon activation

Question 18

What is Indomethacin?

Answer 18

NSAID

Use: Close patent ductus-arteriosus

Question 19

Cyclooxygenase-2 Inhibitors

Answer 19

Celecoxib
Mech: Selectively inhibit COX-2 (inflamm. cells)
Uses: Analgesic, RA, CTDs, muscle strains, soft tissue diseases
SE: Similar to NSAIDs, but less GI disturbance. Increased cardio risk.

Question 20

Acetominophen

Answer 20

Mech: REVERSIBLY weakly inhibits COX. Peripherally inactivated–> MOSTLY CNS effects.
Uses: Antipyretic, analgesic. NO effect on inflammation.
SE: Hepatic necrosis (deplete Glutathione).

Question 21

What prophylaxis can you give to prevent hepatic toxicity w/ Acetaminophen?

Answer 21

N-acetylcysteine
Methinonine
–> Regenerate Glutathione