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ENDO/REPRO > Drugs > Flashcards

Drugs Flashcards

1
Q

-How do androgens act??
-What are 2 important androgens?
-Mayor use?
-Contraindicated?

A

-Androgens enter cells and bind to cytosolic receptors  The hormone-receptor complex enters the nucleus  modulates the expression of target genes.

-Test and DHT

-Hypogonadism males and stimulates grwoth (other uses anemia,osteoporosis–>replaced by other drugs.)

-Cancer of prostate and breast cancer, children, heart disease.

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2
Q

Androgens effects on body (males)?
Diffrences between Testosterone and DHT?

A

-Differentiation of vas deferens, epididymis, seminal vesicles, of internal genitalia not the prostate, growth spurts [penis, bone, RBC, muscle, deepening of voice] closing of epiphysial plates, libido.

-DHT develops the prostate, promotes baldness and sebum.

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3
Q

Oxandrolone

A

Anabolic steroid= Everything same as Testosterone.

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4
Q

Danazol?
Use
SE

A

-Synthetic androgen but has ANTI-GONADOTROPIN (decr GnRH) and ANTI-ESTROGEN effects.
-Used:Endometriosis,Hederitary angioedema
-SE mostly due to incr androgens.

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5
Q

Methyltestosterone??

A

-Androgen recep. agonist.
-hypogonadism and promote development of 2° sex characteristics.
-Virilization–>Female
Male–>Testicular atrophy and closure epiphyseal plates (prematuirly),Incr LDL (heart dis) and decr LDL.

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6
Q

What drugs do you use for prostate cancer(3)?

A

Anti-Androgens:

1.Abiraterone–>inhibits 17 alpha Hydroxylase and 17-20 Lyase (decr steroid sythesis)
AE: Hypokalemia + Hypertension

2.Ketoconazole–> same mechanism as Abiraterone.
AE:Gynecomastia

3.Flutamide/Bicalumide: nonsteroidal competitive inhb in androgen recep.–>DECR STEROID BINDING
Gynecomastia + Sexual dysfunction

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7
Q

Treat for BPH?

A

Tamsulosin (alpha1A specific inhibitor)–>specific for baldder.Alpha 1B is prazosin (vasvular smooth m relax).

Finasteride–>5 alpha reductase inhibitor. Decr DHT–> decr prostate growth. Also given for baldness

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8
Q

Spironolactone (3)??

A

-Used in hypertention and HF, but also used in PCOS

-17α-hydroxylase/17,20-lyaseinhibitor and androgen recep blocker.

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9
Q

What drugs we give in Male sexual dysfunction drugs(2)
Contraindication?

A

-Testosterone

-Phosphodiesterase 5 inhib (Side-nafils)–>AE:flushing,headaches,hypotension.
Contraindicated with nitrates.

Sidenafil works by incr cGMP–>smooth muscle relaxation by inhibiting its degragation.

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10
Q

Peyronies dis. of penis treat.

A

Collagenase injection once erejction resolves.
-Pentoxyfilline

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11
Q

Commonly used regimen for prostate cancer??

A

GnRH agonist(Leuprolide) + Flutamide (anti androgen), Docetaxel (taxane) + prednisone & Mitoxantrone(anti cancer medication)

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12
Q

Hyperstabilize polymerized microtubules prevent mitotic spindle breakdown.

Bind β-tubulin and inhibit its polymerization into microtubules prevent mitotic spindle formation.

A

*All specific for M Phase

Taxanes: Docetaxel, paclitaxel.
AE: Myelosuppression, neuropathy, hypersensitivity

Vinca alkaloids Vincristine, vinblastine.Solid tumors.
cristine–>neurotoxicity
blastine–>myelosupression.

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13
Q

Treat for testicular tumors??

A

Cisplatin:Cross-link DNA.Cell cycle non specific. AE:Fanconi syndrome+Nephrotoxic+Ototoxic,Peripheral Neuropthy

Etoposide (Incr. DNA degradation resulting in cell cycle arrest in S and G2 phases via Top.2 inhibition) “Platinium compound”

Bleomycin(Induces free radical formation breaks in DNA strands.Cell cycle specific for G2 and Mitosis) AE: pulmunary fibrosis and skin hyperpigmentation.

Ifosfamide (cyclophosphamide.Cross link DNA but requieres bioactivation by liver)

Paclitaxel

Vinblastine

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14
Q

How do they work and AE.

Cisplatin:
Paclitaxel:
Docetaxel:
Vinblastine:
Bleomycin:
Etoposide

A

Cisplatin**:Cross-link DNA.Cell cycle non specific. AE:Fanconi syndrome+Nephrotoxic+Ototoxic,Peripheral Neuropthy

Etoposide (Incr. DNA degradation resulting in cell cycle arrest in S and G2 phases via Top.2 inhibition) “Platinium compound”

Bleomycin(Induces free radical formation breaks in DNA strands.Cell cycle specific for G2 and Mitosis) AE: pulmunary fibrosis and skin hyperpigmentation.

Ifosfamide (cyclophosphamide.Cross link DNA but requieres bioactivation by liver)

Paclitaxel

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15
Q

Drugs to treat Genital Herpes
-Mechanism action
-Use
-Resistance? what do you give?
-Adverse effects?

A

-Acyclovir,Famciclovir,Valacyclovir
-Guanosine analogs that are activated only by infected cells via Thymidine kinase.–>fewer side effects
-Inhibits DNA synthesis by chain termination.
-HSV and VZV, NOT efficient for EBV and NO action at all CMV.
-Thymidine kinase mutation
-Obstructive crystalline nephropathy + Acute kideny injury if not adequetly hydrated.
**Foscarnet **(dosent require Thymidine kinase).

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16
Q

Which -ciclovir has better biovalibility?

A

Aciclovir

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17
Q

Treat of Chlamydia/all subtypes ??

A

Adolesnce:Doxycycline

Alternate:Azithromycin
Levofloxacin

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18
Q

Tetracyclines??
-Mechanism
-Why is it used in Chlamydia?
-AE
-Not taking with??

A

-Doxycycline, Tetracycline (-cyclines)
-Bind to A site on 30S in prokaryotes
-Accumulates intracellularly.
-Teeth discoloration,Nephropathy (Doxycycline safe),phototoxixity. Fanconiny syndrome.
-Milk, Anti-acids, irom compounds.

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19
Q

Macrolides?

A

-Azitromycin,Erythromycin, Clarithromycin
-Binds to 50S reversibly (Bacteriostatic)
-Erythro causes diarrhea,Prolonged QT, Eosinphilia.

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20
Q

Levofloxacin type of drug?
-Mechanism
-AE

A

-Fluoroquinolone (-Floxacin)
-Inhibits Topoisomerase 2 (DNA Gyrase) and Top. 4–.DNA stand breaks
-A.E: Tendonitis–> Dont’t give at >60 yrs.athletes,prednisone patients.

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21
Q

Epididymitis treat (3)?

A

Doxycycline, Azitromycin,Levofloxacin
-Caused by Chlamydia

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22
Q

Treat Syphylis?

A

-Penincillin G
-DAla-DAla analog–>inhb transpeptidase (penincillin biding protein)

23
Q

Main treat for Gonorrhea
Chancroid

A

-Ceftriaxone
-Azithromycin

24
Q

Condylomata acuminata treat.?

A

-Imiquinoid (activates immune system)
-Toll like recep 7–>mimmics cytokines

25
Q

What 2 antibiotics are contraindicated in preganancy–>when patient gets UTI/STI?
-What do you give?

A

-Fluoroquinolone and Tetracycline.
-Give Macrolides

26
Q

Prophylaxis for:
Mycobacterium TB
M.Avium

A

-Rifamycin 3-4 months.
-Azithromycin+ Ethambutol

27
Q

Ethambutol

A

-Specific for acid fast organism.
-Inhibits arabinosyltransferase–> decr polymerization of carbohydrates in this bacteria.

AE:Optic nueropathy

28
Q

What drug can be given for infertility that its action depends on the pulses?

Clomiphene diffrence?

A

Gonadorelin
-Antagonist to estrogen receptors in Hypothalamus–> Incr LH and FSH from pituitary.

29
Q

Drugs that cause Disulfiram Recation?

A

1* Generation sulfanuryeas (diabetus)
procarbazine (Hodkin lymphomas),
some chephalosproins,
griseofulvin,
metroniadozole

30
Q

Why does probenecid be given in Syphylis?

Why

A

-Probenecid inhb excretion of penincillin–>incr biovalibility of it–>more effective against syphylis.Used when low penincillins was present–> NOT now

31
Q

DES, Ethylin estraidol,mestranol

A

All estrogen analogs
-Used in estrogen therapy to reduce hot flashes
-Contraindicated in breat cancer, >35 yrs who smoke due to thrombo-embolic events.
-AE: vaginal adenocarcinoma, endometrial cancer

32
Q

Raloxifine
Tamoxifen
Clomiphene

AE

A

-Antagonist in breast and uterus, AGONIST bone–>used in osteoporosis, NO risk for endometrial carcinoma.,Incr risk DVT **
-Antagonist in breast and AGONIST uterus and bone–>used in breast cancer and prevention gynecomastia in Prostate adenocarcinoma INCR RISK FOR ENDOMETRIAL CARCINOMA.Incr DVT Risk**

-Antagonist towards hypothalamus GnRH estrogen recep.–>inibts the negative feedback mechanism.Allowing incr GnRh secretion–>incr LH and FSH–>giving in infertility (promote pregnancy),like PCOS (anovulation).May cause hot flashes,ovarian growth, multiple pregnancies. VIsual disturbensses

33
Q

Endometriosis treat?

A

-Treat based on reducing ovulation (ovary function)
-NSAIDS (pain)
-OCP (progestin)–>
-Danazole–>not used anymore due to androgen side effects and incr intracranial hypertension and edema
-Leuprolide
-Aromatase inhib

34
Q

Treat for Acute Endometritis?

A

-Gentamycin + Clindamycin
or Ampiccilin+ Talobactam

-Empirical treat, to many bacteria present, culture will NOT work.

35
Q

Drug ass with Endometrial Polyps

A

-Tamoxifen (estrogen agonist in endometrium but antagonist in Breast)–>used for breast cancer.

36
Q

Atosiban

A

-Oxytocin antagonist (delay pre-maturity)

37
Q

Tranexamic acid??
Use

A

-Inhibits plasminogen to plasmin
-Control execissive bleeding in females.
Given in Bleeding situations

38
Q

Trastuzumab??
-Meaning on receo it acts?
AE

A

-Used in cancer related with HER2/new over-expression (Breast and Gastric).

Human Epidermal Growth Factor 2
Dilated Cardiomyopathy

39
Q

Exemestane,Anastrozole,Letrozole??
What reaction will it inhibit?

A

Aromatase inhibitors
Given in ER+ Breast cancer in post-menopausal individuals

Remember:
Andostenodione—>Estrone
Testosterone—>Estradiol both by Aromatase

40
Q

Chemotherapies for Breast cancer (4)

A

-Aromatase inhib (-zole)
-Tamixofen
-Trastuzumab
-

41
Q

What type of Breast cancer is Tamixofen used for??

A

-ER/PR recep +

42
Q

Drugs used for

Gestational Hypertension

A

-Hypertensive Moms Love Nifedipine
Hydralazine–>direct vasodilator –>Reflex Tachycardia (may give Beta blocker to prevent it)–>Drug Induced Lupus (Joint pain)
alpha methyl-dopa–> +Direct Coomb Test
Labetolol–>Beta blocker (Beta 1)–>Contraindicated in AV blocks.
Nifedipine—>Block L-type Ca++ chanels–>ANKLE EDEMA

43
Q

Pre-Eclampsia

A

-Magnesium Sulfate (prevents seizure and therefore progressio to Ecmaplsia)
**-Anti-Hypertensive ( possibly being 160/90)
-Prophylaxis;ASPIRIN**–>prevents excessive clot formation due to endothelial damage.
-Definite delivery

*If given and option fisrst thing to do is delivery of fetus and placenta

44
Q

Why Rimfampin reduce estrogen efficacy?

A

-Estrogen is reabsp in intestines and undergoes conjugation in liver via cyt P450–> taking a stimulator

45
Q

Ethinyl estradiol,DES?
Use
Adverse effects
Contraindicated
-Effects on Thyroid h

A

-Synthetic Estrogens
-Primary ovarian insufficency, OCP (along side progestins),treat of dysmenorrhea (alon side progestin–>to prevent ovulation),Hormone replacement therapy
-Post-menopausal bleeding, breast tendernes, incr risk of Endometrial adenocarcinoma (without progesterone–>usually in Hormonal replacement therapy), DES in utero causes adenocarcinoma of vagina <20yrs
-Contraindicated: +ER Breast cancer, Endometriosis, Endometrial Hyperplasia/Adenocarcinoma,Pregnancy,History of DVT, smoker >35 yr of age, uterine fibrinoids,Hepatic disease (metabolized)
-Increases TBG–>INCR TOTAL T3 and T4 but NORMAL FREE T3 and T4 and TSH–>NO thyroid symptoms.

46
Q

Effects of estrogen and progesterone in endometrium?
-What is Progeterone Challenge?

A

-Estrogen–>Stimulates Growth
Progesterone–>Stimulates vascularization and stops growth.

-Administer progesterone and stop suddenly–>if patient bleeds,tells you that endometrium is responding towards estrogen.Eliminate Asherman syndrome and chronic anovulation without estrogen

47
Q

Levonorgestrel, medroxyprogesterone, etonogestrel

A

Progestins (bind to progesterone receptors)
-Contraceprions,Endometrial cancer,Progesterone challenge.

48
Q

Leuprolide,nafarelin,histrelin

-use

A

GnRH agonist
-Pulsatile–>agonist
Continues–>first agonist,later antagonist
-ER+ Breast cancer, Prostate cancer,Endometriosis,Fibrinoids,Pre-cocious puberty—> Continous fashion
-Infertility–>pulsatile

49
Q

Dagirelix
Why is it better than other medications used?

A

GnRH recep antagonist–>acts via Gq (decr IP3)
-Prostate cancer.

-NO start up flare

50
Q

2 Contraceptive mechanism and thir action

Adverse effects

A

1.Estrogen + Progesterones
-Progesterone–>inhibits LH surge (decr GnRH pulses)–> therefore dosen’t permit ovulation.Produces in ednometrium a abn enviroment for implantation and thick mucus so that sperm doen’t enter
-Estrogen decr FSH surge–>supressing ovulation.
2.Progestin alone

-Headaches,edema,hot flashes, More seroius:DVT (ass with estrogen-progestin therapy),MI (obese,smokers,DM,Hypertension),Hepatic adenoma,Cerebrovascular dis

-Comtraindicated: ER+ Breast cancer, Cerebrovascular,HF, Liver dis,history smoking,Fibrinoids,anti-microbials (Rifampin)–>decr concentration.

51
Q

Abortificant medication
-Use with what medication.

A

Mifepristone (anti-progestine)
Ulipristal –>Emergency

-Use along side with misoprostol (PGE1 anolog)–>promotes uterine contraction, normally used with NSAIDS therapy to prevent gastric ulcers

52
Q

Treat for PCOS (6)
-Why do you want this patients to go throught weight loss and treat them with OCP?

A

-Spironolactone (excess adrogen)
Flutamide (excess androgen–>andogen receo inhibitor)
**Finasteride (androgen effects)
OCP (disrupt LH and FSH levels)
Metformin (DM)
Clomiphene (estrogen inhibitor at Hypothalamus–>promote LH and FSH rels.–>help in ovulation.)**Treat used if patient wants to get pregnant.

-Weight loss–>decr estrone formation–>decr in negative feedback towards FSH–>normolizing FSH levels
OCP–>reduce risk in endometrial cancer anovulatory cycles) due to unopossed estrogen esposure.

53
Q

Ulipristal, a selective progesterone receptor modulator, acts as an emergency contraceptive by inhibiting or delaying ovulation up to 120 hours (5 days) following intercourse. This is commonly the first-line treatment for emergency contraception, but it is less effective for patients with obesity (body mass index >30 kg/m2).

Hormonal methods of emergency contraception such as levonorgestrel (Plan B) act as emergency contraception partly by delaying ovulation up to 72 hours (3 days) following intercourse. This method is less effective in patients with obesity (body mass index >30 kg/m2).

A
54
Q

Side effects of Danazol?

A

-Intra-cranial Hypertension,Edema,Maculanization

ENDO/REPRO (10 decks)

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