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D&T 4: Exam 1 > Drugs > Flashcards

Flashcards in Drugs Deck (90):
1

Methyltestosterone, Fluoxytestosterone

17a-hydroxylated testosterone analogs that are orally effective; used to tx hypogonadism and metastatic breast cancer IN WOMEN

CIs: Prostate cancer
Male Breast cancer
Pregnancy

ADRs: Choelstatatic hepatitis/ HEPATOTOXICITY
Inhibition of Vit-K dep. coag factors
Hepatic cancer
Edema, HTN

2

Danazol

Suppresses the pre-ovulatory surge in FSH and LH
=>>anovulation and decreased androgens

Tx: ***Endometriosis, fibrocystic breast disease, hereditary angioedema

ADRs: Acne, *weight gain, thrombosis, mood swings
-Acts as a weak androgen

CIs: Pregnancy, Breast feeding

3

Stanazol

17a-derivative of testosterone; raises C1 INH and CF

Tx: Hereditary Angioedema

ADRs: **Hepatotoxicity, decreased Vit-K dependent factors, acne, irreversible baldness in women

CIs: Pregnancy
Male Prostate or Breast Cancer
Female Breast Cancer w/ Hypercalcemia

4

Oxandrolone

High anabolic activity and little androgenic activity; used for weight gain post-surgery or trauma

ADRs: Irritability, edema, HTN

CIs: Breast cancer, prostate cancer, pregnancy

5

Finasteride, Dutasteride

Competitive inhibitors of 5a-reductase =>> decreased levels of DHT
*DHT normally works to increase prostatic stromal cell creation and inhibit epithelial apoptosis

-Used in conj. w/ tamsulosin in BPH; also used to tx male pattern baldness

ADRs: Gynecomastia; PREGGERS WOMEN SHOULDNT EVEN TOUCH A PILL

6

Leuprolide

GnRH agonist resulting in down-regulation of FSH and LH =>> decreased levels of testosterone

*Used to tx prostate cancer and endometriosis

ADRs: Hot flashes; night sweats; gynecomastia, thrombosis

7

Flutamide

Interferes w/ testosterone binding to target tissues; indirectly =>> increased testosterone in the bloodstream

Tx: Prostate cancer, *Acne

ADRs: Hepatotoxicity; gynecomastia

8

Testosterone Analogs

Administered IM or via a topical gel; undergoes extensive first-pass metabolism

Gel should not be applied directly to testicles ya dingus

Remove if going into MRI (contains Al3+)

May cause hirsutism on female partner

FDA BLACK BOX WARNING

9

Conjugated estrogens

Mostly used for post-menopausal therapy

10

Ethinyl estradiol

Main estrogen used in OCPs for young women; also has an increased dose than conjugated estrogens

11

Monophasic combination OCP

21 days of estrogen and progesterone; 7 days or iron

-Should have 13 periods; roughly normal

-Lack of a period indicates failure

12

Diphasic or Triphasic combination pills

Usually lower the ADRs of OCPs; triphasic is most common

13

Mircette

Only two days of placebo before 5 days of low estrogen dose; idea is to decrease the amount of estrogen withdrawal effects

-Decreased headaches, bloating, menstrual pain

14

Yaz

Contains estrogen and drospirenone***

-Improves symptoms of premenstrual dysphoric disorder

Contains...
**Drospirenone is a spironolactone derivative and is capable of causing hyperkalemia
=>>avoid in pts. w/ renal failure, on other drugs that cause hyperkalemia

15

Seasonale

Levonorgestrol combo taken for 80ish days that reduces periods to once every seasonish

16

Lybrel

Low dose OCP taken every day of the year

17

Xulane Patch

High dose of estrogen that is highly assoc. w/ skin rash and thrombosis BUT can avoid the first pass hepatic effects

18

Drugs with the most progestational and androgenic activity

Levonorgestrol and Norgestrol

19

Progestin-only drugs w/ lowest androgenic activity

Desogestrel, Norgestimate, Gestedone, Drosperinone

20

Effects of COCs

-Prevention of the midcycle LH and FSH surge

-Thickens endocervical fluid

-Stabilizes an unsuitable endometrium for implantation

21

OCP ADRs

Nausea

Headache

Thrombosis (increased platelet aggregation; increased vitamin-k dependent factors)

HTN

Weight gain

Increased Risk for:

*Cholestatic jaundice =>> possible gall stones

-Stroke, MI, thromboembolism

-Breast cancer

22

Non-contraceptive benefits to OCPs

Increased bone density

Decreased acne

Decreased epithelial ovarian cancer

Tx polycystic ovary disease

23

Adjustment of Estrogen Dose in OCP

Adjust to Lower if: N/V, migraines, HTN, hypermenorrhea

Adjust to higher if: Hot flashes, hypomenorrhea

24

Adjustment of progesterone dose in OCP

Adjust to lower if depression or reduced breast size

Adjust to higher if late bleeding or hypermenorrhea

25

Adjustment of androgenic activity in OCP

Adjust to lower if acne, hirsutism, or weight gain

26

Non-nursing mothers w/ OCPs

Wait 4 weeks; anything less than 2 can def. cause thrombosis

27

CYP induction and OCPs

Increased metabolism; increase dose w/

-Smokers

-Carbamazepine

-Phenytoin

-Rifampin

-Erythromycin

-Penicillin V

-Tetracycline

-Overweight pts. too****

28

Situations for minipill use

Nursing mothers

Women w/ CIs for COCs (smoking, history of thrombophlebitis)

-Migraines, Depression

These are not as effective as COCs but still work 80% well
***Missing one tablet =>> THERAPEUTIC FAILURE

29

Medroxyprogesterone Acetate

Injectable OCP once/3months that highly effective by impairing LH release and causing endometrial atrophy
-Delay in fertility after stopping

***Causes weight gain and severe osteoporosis; DO NOT USE >2 YRS

30

Paragard

Copper containing IUD; toxic to sperm

31

Octoxynol-9 or nonoxynol-9

Spermicide gel that destroys their cell membrane; additives can induce allergy

32

Estrogen therapy in post-menopausal women

Only recommended in women who have gone hysterectomy since there is no risk of endometrial cancer

33

Bazedoxifine

Estrogen agonist at the bone and antagonist at the uterus; approved for tx of vasomotor sx and osteoporosis

Long-term thrombosis risk unknown

34

2 drugs that cannot cross the placenta

Insulin and heparin

35

Grey baby syndrome

Infant presents w/ grey cyanosis, circulatory collapse, hypothermia, and abdominal distention

-Due to maternal consumption of chloramphenicol

36

Treatment for UTI in pregnancy

Nitrofurantoin, penicillin, possible bactrim

37

Sinusitis tx in pregnant woman

Bactrim, penicillin, azithromycin

38

Maternal hyperthyroidism

Must treat or fetus will die

Propylthiouracil, carbimazole, methimazole

-Avoid radioablation therapy

-There is a chance the baby will have hypothyroidism and a goiter

39

Maintenance of pre-eclampsia

Methlydopa or hydralazine until fetus is delivered

40

Maternal HTN

Tx: methyldopa, hydralazine, labetalol, Ca2+ blockers

-Avoid ACEIs, ARBs, diuretics, clonidine

41

Fetal hydantoin syndrome

Craniofacial abnormalities, cadiac defects, genitourinary defects

-Tx mothers w/ seizures w/ either carbamazepine or Valproate (still a risk for teratogensis!) because seizures bad

-Make sure to supplement folic acid!

42

Hyperemesis gravidarium

Severe form of nausea and vomiting requiring hospitalization due to dehydration

-Attempt non-drug therapy at first (small meals, hydration, B6)

-Odansetron next

43

Tx of maternal depression

Sertaline is safest SSRI but still some teratogenic risk

Paxil➡️ VSDs

44

Iodothyronine 5'-deiodonase

Converts T4 to T3; two subtypes

D1- liver, kidney, thyroid; responsible for most circulating T3
-highest activity in liver; CYP450 inducers will increase activation

D2- brain, pituitary, skeletal and cardiac muscle; not affected by propylthiouracil

45

Levothyroxine

T4

Oral drug used for Hashitmoto's (DOC), suppression of TSH in ademoma or hyperplasia

IV drug used for life-threatening myxedema comma

⭐️⭐️⭐️⭐️⭐️Inhibits D1
as does Amiodarone


-Interacts w/ cholestyramine, calcium carbonate (decreased conc.)
estrogen (increases TBG so increase dose)
glucocorticoids (decreases TBG)
propylthiouracil

ADRs: cardiac arrhythmia, palpitations

46

Liothyronine

T3; has decreased duration of action compared to levothyroxine

Use in pts. With a 5-deiodinase deficiency

47

Propylthiouracil

Inhibits iodonation of tyrosine residues, coupling to form iodothyronine, and peripheral D1

-Preferred hyperthyroidism tx during pregnancy due to less birth defects

ADRs: Hepatotoxicity (potential failure =>>BLACK BOX), nephrotoxicity

48

Methimazole

Inhibits the iodination of tyrosine residues and coupling of DIT or MIT; more effective drug than Propylthiouracil

*Propylthiouracil and methimazole both used prior to thyroidectomy

ADRs: agranulocytosis; aplastic anemia

49

Iodine 131

Used to tx. hyperthyroidisms; may induce hypothyroidism due to excess damage

50

Iodide

Reduces vascularity prior to thyroidectomy; blocks radioiodine uptake in nuclear accidents

Helps prevent thyroid storm

51

Somatropin

GH analog used to tx. pituitary dwarfism; ineffective after epiphyseal plates have closed

-Can also be used for Turner Syndrome, Prader-Willi

ADRs: May see increased ICP early on

52

Laron Dwarfism

Genetic mutation in the GH receptor; tx. w/ IGF-1

ADRs: hypoglycemia (administer right after meal to avoid)

53

Octreotide, Lanreotide

Somatostatin analogs used to inhibit GH secretion at the pituitary

-Used to tx. acromegaly and gigantism

ADRs: N/V, vomiting, diarrhea, cholestatic jaundice

54

Pegvisomant

Competitive GH receptor antagonist used to decrease the levels of IGF-1 in pts.; also indicated for acromegaly

55

Cabergoline

More effective and longer lasting bromocriptine (dopamine agonist); used to tx. prolactinemia

ADRs: Possible N/V; valvular disease

56

Protirelin

Synthetic TRH used for diagnostic purposes

Increase in TSH = problem in hypothalamus

No increase = problem in pituitary

57

Cosyntropin

ACTH analog used for diagnostic purposes

58

Synthetic hCG

Promotes ovulation in anovulatory women and sexual development in male infertility and cryptorchidism

*Basically works like LH

59

Menotropin

Received from urine of postmenopausal women and contains degraded produces of FSH and LH

-Stimulates ovarian follicle development in females and spermatogenesis in males

*Basically works like FSH

**Urofollitropin is the same but w/ the LH REMOVED

60

Clomiphene

Estrogen receptor antagonist at the level of the hypothalamus that
=>>Increased GnRH secretion

-Used to tx. infertility due to PCOS

ADRs: Antiestrogenic effects on developing follicle and possible development of ovarian cysts

61

Leuprolide, Gosarelin, Nafarelin, Histarelin

GnRH analogs w/ long half lives and Increase receptor binding affinity ultimately leading to a Downregulation of the GnRH receptor and ultimately decrease activity

Uses: Enometriosis, prostate cancer, uterine cancer, breast cancer, precocious puberty

ADRs: Hot flashes, osteoporosis, vaginal dryness, erectile dysfnxn

62

Flutamide, Biclutamide

Androgen receptor antagonist given alongside leuprolide

Tx: Prostate cancer

-If given ALONE, will increase LH synthesis and worsen cancer

ADRs: Black box for reversible liver damage

63

Desmopressin

Increased activity at the principal cells but decreased vasopressor activity when compared to vasopressin

*Also stimulates prod. of vWF and Factor VIII and is therefore indicated for the tx. of von-Willebrand's disease

ADRs: Possible water intoxication because damn this shit works good

Chlorpropramide and Chlorprommazine sensitize tubules; Li 2+ will inhibit fnxn

64

Tx for nephrogenic DI

Thiazides

65

Amiloride

Blocks Li+ uptake in the Na+ co-transported in the PCT; reverse Li+ induced nephrogenic DI

66

Conivaptan, tolvaptan

V1/V2 receptor antagonists used to tx. euvolemic hyponatremia assoc. w/ SIADH

67

Best imaging test to exclude pituitary apoplexy (sheehan's)

MRI w/ and w/o contrast

Use CT w/o contrast if MRI is unavailable

68

Best test for imaging in Grave's Disease

I123 nuclear medicine scan w/ examination of radioiodide uptake (should be increased diffusely)

69

You discover a cold nodule on thyroid scan, what should you do next?

US to id whether it is a thyroid cyst or tumor

70

Imaging tests for hyperparathyroidism

US, sestamibi scan, SPECT/CT, enhanced CT

71

Rapid acting Insulin

Aspart =>> FASTEST; onset in 5 mins
-Aspartate subs. for pro

Lispro and Glusline 15ish mins

Compatible w/ NPH

72

Long Acting Insulin

Have no peak; love you real long time and provides the most CONSISTENT levels of insulin

Detemir- increased plasma protein binding; deletion of AA on B-chain

Degludec lasts 42 hrs

73

NPH

Closest to normal insulin; contains protamine

74

Pramlintide

Amylin analog that inhibits glucagon secretion, decreases hepatic gluconeogenesis, and delays gastric emptying

ADRs: Hypoglycemia (do not mix w/ insulin in same syringe);

75

Chlorpropamide

Sulphonylurea that stimulates insulin release by decreasing the conductance of K+ thru the ATP-activated channel
=>>increased intracellular Ca2+ and insulin release

Also decreases hepatic gluconeogenesis and increases GLUT channels peripherally

CYP metabolized

Interacts w/ ADH =>> water retention =>> weight gain
-Can also use this in pts. w/ diabetes insipidus who cannot tolerate desmopressin

76

Glyburide Glimepride

2nd generation sulphonylurea that does not cause weight gain or edema

77

Repaglinide, Nateglinide

Metaglinides that stimulate insulin release by causing cellular depolarization =>> increased intracellular Ca2+ in B-pancreatic cells =>>insulin release
-Structurally different from sulphonylureas

-used in combo w/ metformin; cleared in 4 hrs so use multiple times/day

CYP metabolized

ADRs: hypoglycemia, don't use w/ DKA

78

Metformin

Decreases hepatic gluconeogenesis, increases peripheral sensitivity to insulin, and decreases hepatic glucose absorption

-Has no affect on insulin secretion

Pros: No hypoglycemia, no weight gain, helps decrease lipids

ADRs: Cramping, flatulence, decreased Vit-B12 absorption, lactic acidosis w/ alcohol consumption

**Also used for infertility related to obesity and PCOS
=>>Decrease androgen levels and inhibit synthesis of sex-hormone binding globulins

79

Acarbose, Miglitol

Inhibitor of intestinal amylase and a-glucosidase; reduces absorption of starches in the intestines (***does not reach bloodstream)

-Must take right before meal

ADRs: Flatulence, abdominal pain
*Acarbose =>> MONITOR ALT


80

Pioglitazone, Rosiglitazone

Thialidizones

Increases glucose uptake into skeletal muscle; activates PPARy receptors increasing insulin responsive genes; decreases hepatic gluconeogenesis

-Works outside of pancreas; does not stimulate insulin release

ADRs: Elevated transaminases; edema and weight gain

****Worsens CHF and causes edema (BLACK BOX)




81

Exenatide; Liraglutide

GLP-1 hormone secreted after a meal

Suppresses compensatory glucagon that normally follows insulin release and simulates glucose-dependent insulin release

ADRs: Hypoglycemia; pancreatitis
BLACK BOX WARNING : DO NOT USE W/ HISTORY OF THYROID CANCER

82

Alogliptan, Saxagliptan, Sitagliptan

Dipeptidyl peptidase IV inhibitors

Increases GLP-1 t^1/2

ADRs: Hypoglycemia; decrease dose at first if also on sulphonylurea or megatilinides

-Renal impairment, liver damage

83

Canaglifozin, Dapaglifozin

SGLT-2 inhibitor in the PCT; increases renal excretion of glucose

-Can be monotherapy w/ diet and exercise

ADRs: Increases UTI rate; hypotension; hyperkalemia w/ K+-sparing diuretics

-Do not give w/ renal impairment

84

Diazoxide

Given orally to raise blood glucose

Tx for insulinoma

85

Progestins

Pregnane- similar to progesterone; includes Medroxyprogesterone acetate

Estrane- similar to 19-nortestosterone; includes. Norethedrone also

Gonane- similar to Norgestrel; includes Norgestimate

Drospirenone also in this class but similar to mineralcorticoids

86

Lithium effect on T4

Inhibits release

87

Agents that reduce thyroxine bioavailability

Calcium carbonate

Cholestyramine

Aluminum hydroxide

88

Demeclocycline

️Inhibits the activity of vasopressin on the collecting ducts

89

DOC for DKA

Short acting insulin; NEVER STOP INFUSION

Normal saline, possibly stronger after 1 hr

D5W If glucose

90

Cerebral edema in DKA

Occurs due to prod. Of immunogenicity osmols across the BBB during DKA; once saline is added, can cross over and produce fatal swelling