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Flashcards in Random pharmacology Deck (82):
1

Fulvestrant

- A "pure" estrogen antagonist
- Associated with a much lower risk of causing endometrial pathology, including cancer than raloxifene or toremifene

2

Ranolazine

- MECHANISM: inhibits late phase of sodium current thereby reducing diastolic wall tension and oxygen consumption; does not affect HR or contractility
- CLINICAL USE: angina refractory to other medical therapies
- ADVERSE EFFECTS: constipation, dizziness, headache, nausea, QT prolongation

3

Cinacalcet

- MECHANISM: sensitizes Ca2+ sensing receptor (CaSR) in parathyroid gland to circulating Ca2+, leads to decrease in PTH
- CLINICAL USE: primary or secondary hyperparathyroidism
- ADVERSE EFFECTS: hypocalcemia

4

Orlistat

- MECHANISM: inhibits gastric and pancreatic lipase and leads to a decrease in breakdown and absorption of dietary fats
- CLINICAL USE: weight loss
- ADVERSE EFFECTS: steatorrhea, decreased absorption of fat-soluble vitamins

5

Ursodiol (ursodeoxycholic acid)

- MECHANISM: nontoxic bile acid that increases bile secretion and decreases cholesterol secretion and absorption
- CLINICAL USE: primary biliary cirrhosis, gallstone prevention or dissolution

6

Cladribine

- MECHANISM: purine analog that works through multiple mechanisms (eg inhibition of DNA polymerase, DNA strand breaks); an antimetabolite
- CLINICAL USE: hairy cell leukemia
- ADVERSE EFFECTS: myelosuppression, nephrotoxicity, neurotoxicity

7

Cytarabine (arabinofuranosyl cytidine)

- MECHANISM: pyrimidine analog that leads to the inhibition of DNA polymerase; an antimetabolite
- CLINICAL USE: leukemias (AML), lymphomas
- ADVERSE EFFECTS: myelosuppression with megaloblastic anemia ("CYTarabine causes panCYTopenia")

8

Nitrosureas (carmustine, lomustine, semustine, streptozocin)

- MECHANSIM: requires bioactivation; works as an alkylating agent; crosses blood brain barrier into the CNS where it crosslinks DNA
- CLINICAL USE: brain tumors (including glioblastoma multiforme)
- ADVERSE EFFECTS: CNS toxicity (convulsions, dizziness, ataxia)

9

Erlotinib

- MECHANISM: EGFR tyrosine kinase inhibitor
- CLINICAL USE: non-small cell lung cancer
- ADVERSE EFFECTS: rash

10

Cetuximab

- MECHANISM: monoclonal antibody against EGFR
- CLINICAL USE: stage IV colorectal cancer (wild-type KRAS), head and neck cancer
- ADVERSE EFFECTS: rash, elevated LFTs, diarrhea

11

Vemurafenib

- MECHANISM: small molecule inhibitor of BRAF oncogene (+) melanoma
- CLINICAL USE: metastatic melanoma

12

Leflunomide

- MECHANISM: reversibly inhibits dihydroorate dehydrogenase, preventing pyrimidine synthesis; suppresses T cell proliferation
- CLINCIAL USE: rheumatoid arthritis, psoriatic arthritis
- ADVERSE EFFECTS: diarrhea, hypertension, hepatotoxicity, teratogenicity

13

Teriparatide

- MECHANISM: recombinant PTH analog given subcutaneously daily, increases osteoblastic acitivity
- CLINICAL USE: osteoporosis; causes increase in bone growth compared to antiresorptive therapies (eg bisphosphonates)
- ADVERSE EFFECTS: transient hypercalcemia

14

Etanercept

- MECHANISM: TNF-alpha inhibitor; fusion protein (receptor for TNF-alpha + IgG1, Fc), produced by recombinant DNA; acts as a TNF decoy receptor
- CLINICAL USE: rheumatoid arthritis, psoriasis, ankylosing spondylitis

15

Infliximab, adalimumab

- MECHANSIM: TNF-alpha inhibitor; anti-TNF-alpha monoclonal antibody
- CLINICAL USE: inflammatory bowel disease, rheumatoid arthritis, psoriasis, ankylosing spondylitis

16

Rasburicase

- MECHANISM: recombinant uricase that catalyzes metabolism of uric acid to allantoin
- CLINICAL USE: prevention and treatment of tumor lysis syndrome

17

Cyclobenzaprine

- MECHANISM: centrally acting skeletal muscle relaxant; structurally related to TCAs, similar to anticholinergic side effects
- CLINICAL USE: muscle spasms

18

Varenicline

- Atypical antidepressant
- Nicotinic ACh receptor partial agonist
- Used for smoking cessation
- TOXICITY: sleep disturbance

19

Clomiphene

- Selective estrogen receptor modulator
- Antagonist at estrogen receptors in hypothalamus
- Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation
- Used to treat infertility due to anovulation (eg PCOS)
May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

20

Tamoxifen

- Selective estrogen receptor modulator
- Antagonist at breast
- Agonist at bone, uterus
- Increase risk of thromboembolic events and endometrial cancer
- Used to treat and prevent recurrence of ER/PR (+) breast cancer

21

Raloxifene

- Selective estrogen receptor modulator
- Antagonist at breast, uterus
- Agonist at bone
- Increase risk of thromboembolic events but no increased risk of endometrial cancer (vs tamoxifen)
- Used primarily to treat osteoporosis

22

Anastrozole, letrozole, exemestane

- Aromatase inhibitor
- MECHANISM: inhibit peripheral conversion of androgens to estrogens
- CLINICAL USE: ER(+) breast cancer in postmenopausal women

23

Mifepristone, ulipristal

- Antiprogestin
- MECHANISM: competitive inhibitors of progestins at progesterone receptors
- CLINICAL USE: termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal)

24

Terbutaline, ritodrine

- Beta-2 agonists that relax the uterus
- Used to decrease contraction frequency in women during labor

25

Danazol

- MECHANISM: synthetic androgen that acts as partial agonist at androgen receptor
- CLINICAL USE: endometriosis, hereditary angioedema
- ADVERSE EFFECTS: weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels, hepatotoxicity

26

Minoxidil

- MECHANISM: direct arteriolar vasodilator
- CLINICAL USE: androgenetic alopecia, severe refractory hypertension

27

Bosentan

- Pulmonary hypertension drug
- MECHANISM: competitively antagonizes endothelin-1 receptors which leads to a decrease in pulmonary vascular resistance
- CLINICAL NOTES: hepatotoxic (monitor LFTs)

28

Sildenafil

- MECHANISM: inihibits cGMP PDE-5 and prolongs vasodilatory effect of NO
- CLINICAL NOTES: used for pulmonary hypertension as well as erectile dysfunction

29

Epoprostenol, iloprost

- Pulmonary hypertension drug
- MECHANISM: PGI2 (prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds, also inhibits platelet aggregation
- ADVERSE EFFECTS: flushing, jaw pain

30

Fluticasone, budesonide

- Inhaled corticosteroids used for asthma
- Inhibit synthesis of virtually all cytokines
- Inactivate NF-KB , the transcription factor that induces production of TNF-alpha and other inflammatory agents
- 1st line therapy for chronic asthma

31

Omalizumab

- Anti-IgE monoclonal therapy for asthma
- Binds mostly unbound serum IgE and blocks binding to FcERI
- Used in allergic asthma with increased IgE levels resistant to inhaled steroids and long acting beta-2 agonists
- ADVERSE EFFECTS: anaphylaxis (mostly occurs on initial dose)

32

Tesamorelin

- GHRH analog
- Used to treat HIV-associated lipodystrophy

33

Glycyrrhetic acid

Inhibits aldosterone synthase, which normally converts corticosterone to aldosterone and cortisol to cortisone

34

Pegvisomant

Growth hormone receptor antagonist used to treat acromegaly

35

Hyoscyamine, dicyclomine

- Muscarinic antagonist
- GI
- Antispasmodic for irritable bowel syndrome

36

Oxybutynin, solifenacin, tolterodine

- Muscarinic antagonist
- Genitourinary
- Reduce bladder spasm and urge urinary incontinence (overactive bladder)

37

Adverse effects of non-dihydropyridine Ca2+ blockers

- Cardiac depression
- AV block
- Hyperprolactinemia
- Constipation

38

Adverse effects of dihydropyridine Ca2+ blockers

- Peripheral edema
- Flushing
- Dizziness
- Gingival hyperplasia

39

Pindolol and acebutolol

Partial β agonists contraindicated in angina

40

Which lipid lowering agent is associated with hyperuricemia

Niacin (B3)

41

Which lipid-lowering agents ↑ triglycerides

Bile acid resins (cholestyramine, colestipol, colesevelam)

42

Adverse effects of thionamides

- Skin rash
- Agranulocytosis
- Aplastic anemia
- Hepatotoxicity
- Methimazole is a possible teratogen (can cause aplasia cutis)

43

GH used to treat

- GH deficiency
- Turner syndrome

44

What does CUSHINGOID stand for

- C → cataracts
- U → ulcers
- S → striae, skin thinning
- H → hypertension, hirsutism
- I → immunosuppression, infection
- N → necrosis of femoral heads
- G → glucose elevation
- O → osteoporosis, obesity
- I → impaired wound healing
- D → depression/ mood changes

45

Fludricortisone can cause what skin changes

Those associated with glucocorticoids + hyperpigmentation

46

Adverse effects of proton pump inhibitors

- ↑ risk of C difficile infection
- Pneumonia
- ↓ serum Mg2+ with long term use

47

Adverse effects of aluminum hydroxide

- Constipation and hypophosphatemia
- Proximal muscle weakness
- Osteodystrophy
- Seizures

48

Adverse effects of calcium carbonate

- Hypercalcemia (milk-alkali syndrome)
- Rebound acid ↑

49

Adverse effects of magnesium hydroxide

- Diarrhea
- Hyporeflexia
- Hypotension
- Cardiac arrest

50

Adverse effects of sulfasalazine

- Malaise
- Nausea
- Sulfonamide toxicity
- Reversible oligospermia

51

Adverse effects of ondansetron

- Headache
- Constipation
- QT prolongation

52

Adverse effects of ADP receptor inhibitors

- Neutropenia (ticlopidine)
- TTP

53

Cilostazol, dipyridamole

- MECHANISM: phosphodiesterase III inhibitor; ↑ cAMP in platelets, resulting in inhibition of platelet aggregation; vasodilators
- CLINICAL USE: intermittent claudication, coronary vasodilation, prevention of stroke or TIAs (combined with aspirin), angina prophylaxis
- ADVERSE EFFECTS: nausea, headache, facial flushing, hypotension, abdominal pain

54

Azathioprine and 6-mercaptopurine are activated by what enzyme

HGPRT

55

Clinical use of azathioprine and 6-mercaptopurine

- Preventing organ rejection, rheumatoid arthritis, IBD, SLE
- Used to wean patients off steroids in chronic disease and to treat steroid-refractory chronic disease

56

Hemorrhagic cystitis caused by cyclophosphamide and isofamide can be prevented with what

Mesna and N-acetylcysteine. Thiol group binds to toxic metabolites.

57

Used for treatment of c-KIT GI stromal tumors

Imantib

58

Clinical uses of rituximab

- Non-Hodgkin lymphoma
- CLL
- ITP
- Rheumatoid arthritis

59

Mannitol

- MECHANISM: osmotic diuretic; ↑ tubular fluid osmolarity → ↑ urine flow, ↓ intracranial/ intraocular pressure
- CLINICAL USE: drug overdose, elevated intracranial/intraocular pressure
- ADVERSE EFFECTS: pulmonary edema, dehydration
- Contraindicated in anuria, HF

60

Contraindications of mannitol

- Anuria
- HF

61

Loop diuretics have what effect on the medulla

Abolish hypertonicity of medulla, preventing concentration of urine

62

Loop diuretics stimulate release of

Stimulate PGE release (vasodilatory effect on afferent arteriole)

63

What effect do loop diuretics have on Ca2+

↑ Ca2+ excretion

64

Adverse effects of loop diuretics

- Ototoxicity
- Hypokalemia
- Dehydration
- Allergy (sulfa)/ metabolic Alkalosis
- Nephritis (interstitial)
- Gout

"OH DANG"

65

What toxicity is more pronounced in ethacrynic acid than loop diuretics in general

Ototoxicity

66

Potassium sparing diuretics

- Spironolactone and eplerenone; triamterene and amilioride
- Spironolactone and eplerenone → competitive aldosterone receptor antagonists in cortical collecting tubule
- Tiramterene and amiloride → act at the same part of the tubule by blocking Na+ channels in the cortical collecting tubule

67

Diuretics that ↓ pH

- Carbonic anhydrase inhibitors: ↓ HCO3- reabsorption
- K+ sparing: aldosterone blockade prevents K+ secretion and H+ secretion → hyperkalemia additionally leads to K+ entering all cells (via H+/K+ exchanger) in exchange for H+ exiting cells

68

Diuretics that ↑ pH

Loop diuretics and thiazides cause alkalemia through several mechanisms
- Volume contraction → ↑ AT II → ↑ Na+/H+ exchanger in PCT → ↑ HCO3- reabsorption ("contraction alkalosis")
- K+ loss leads to K+ exiting all cells (via H+/K+ exchanger) in exchange for H+ entering cells
- In low K+ states, H+ (rather than K+) is exchanged for Na+ in cortical collecting tubule → alkalosis and "paradoxical aciduria"

69

Adverse effects of ACE inhibitors

- Cough
- Angioedema (↑ bradykinin; contraindicated in C1 esterase inhibitor deficiency)
- Teratogen (fetal renal malformations)
- ↑ Creatinine (↓ GFR by preventing ATII mediated constriction of efferent arterioles)
- Hyperkalemia
- Hypotension
- Used with caution in bilateral renal artery stenosis because ACE inhibtors will further ↓ GFR → renal failure

70

Angiotensin II receptor blockers

Losartan, candesartan, valsartan

71

Clinical use of leuprolide

- Uterine fibroids
- Endometriosis
- Precocious puberty
- Prostate cancer
- Infertility

72

Name estrogens

- Ethinyl estradiol
- DES
- Mestranol

73

Clinical use of estrogens

- Hypogonadism or ovarian failure
- Menstrual abnormalities
- Hormone replacement therapy in postmenopausal women
- Use in men with androgen dependent prostate cancer

74

Adverse effects of estrogens

- ↑ risk of endometrial cancer
- Bleeding in postmenopausal women
- Clear cell adenocarcinoma of vagina in females exposed to DES in utero
- ↑ risk of thrombi

75

Name progestins

- Levonorgestrel
- Medroxyprogesterone
- Etonogestrel
- Norethindrone
- Megestrol

76

Mechanism of progestins

- Bind progesterone receptors
- ↓ growth and ↑ vascularization of endometrium
- Thicken cervical mucus

77

Progestin challenge

Presence of withdrawal bleeding excludes anatomic defects (eg Asherman syndrome) and chronic anovulation without estrogen

78

Mechanism of combined contraception

- Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge
- No estrogen surge → no LH surge → no ovulation
- Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus
- Progestins also inhibit endometrial proliferation → endometrium is less suitable to the implantation of an embryo

79

What can stimulate anabolism to promote recovery after burn or injury

Testosterone or methyltestosterone

80

What causes premature closure of epiphyseal plates

Testosterone or methyltestosterone

81

Used for PCOS to reduce androgenic symptoms

Ketoconazole → inhibits steroid synthesis (17,20-desmolase)

Spironolactone → inhibits steroid binding, 17alpha-hydroxylase, and 17,20-desmolase

82

Minoxidil

- MECHANISM: direct arteriolar vasodilator
- CLINICAL USE: androgenetic alopecia, severe refractory hypertension