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Drugs Flashcards

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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?

Study These Flashcards
A

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

23
Q

Main treat for Gonorrhea
Chancroid

Study These Flashcards
A

-Ceftriaxone
-Azithromycin

24
Q

Condylomata acuminata treat.?

Study These Flashcards
A

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

25
What 2 antibiotics are contraindicated in preganancy-->when patient gets UTI/STI? -What do you give?
-Fluoroquinolone and Tetracycline. -Give Macrolides
26
Prophylaxis for: Mycobacterium TB M.Avium
-Rifamycin 3-4 months. -Azithromycin+ Ethambutol
27
Ethambutol
-Specific for acid fast organism. -Inhibits arabinosyltransferase--> decr polymerization of carbohydrates in this bacteria. AE:Optic nueropathy
28
What drug can be given for infertility that its action depends on the pulses? Clomiphene diffrence?
Gonadorelin -Antagonist to estrogen receptors in Hypothalamus--> Incr LH and FSH from pituitary.
29
Drugs that cause Disulfiram Recation?
**1* Generation sulfanuryeas (diabetus) procarbazine (Hodkin lymphomas), some chephalosproins, griseofulvin, metroniadozole**
30
Why does probenecid be given in Syphylis? | Why
-Probenecid inhb excretion of penincillin-->incr biovalibility of it-->more effective against syphylis.Used when low penincillins was present--> NOT now
31
DES, Ethylin estraidol,mestranol
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
Raloxifine Tamoxifen Clomiphene AE
-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
Endometriosis treat?
-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
Treat for Acute Endometritis?
-Gentamycin + Clindamycin or Ampiccilin+ Talobactam -Empirical treat, to many bacteria present, culture will NOT work.
35
Drug ass with Endometrial Polyps
-Tamoxifen (estrogen agonist in endometrium but antagonist in Breast)-->used for breast cancer.
36
Atosiban
-Oxytocin antagonist (delay pre-maturity)
37
Tranexamic acid?? Use
-Inhibits plasminogen to plasmin -Control execissive bleeding in females. Given in Bleeding situations
38
Trastuzumab?? -Meaning on receo it acts? AE
-Used in cancer related with HER2/new over-expression (Breast and Gastric). Human Epidermal Growth Factor 2 **Dilated Cardiomyopathy**
39
Exemestane,Anastrozole,Letrozole?? What reaction will it inhibit?
Aromatase inhibitors Given in ER+ Breast cancer in post-menopausal individuals Remember: Andostenodione--->Estrone Testosterone--->Estradiol both by Aromatase
40
Chemotherapies for Breast cancer (4)
-Aromatase inhib (-zole) -Tamixofen -Trastuzumab -
41
What type of Breast cancer is Tamixofen used for??
-ER/PR recep +
42
# Drugs used for Gestational Hypertension
**-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
Pre-Eclampsia
-**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
Why Rimfampin reduce estrogen efficacy?
-Estrogen is reabsp in intestines and undergoes conjugation in liver via cyt P450--> taking a stimulator
45
Ethinyl estradiol,DES? Use Adverse effects Contraindicated -Effects on Thyroid h
-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
Effects of estrogen and progesterone in endometrium? -What is Progeterone Challenge?
-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
Levonorgestrel, medroxyprogesterone, etonogestrel
Progestins (bind to progesterone receptors) -Contraceprions,Endometrial cancer,Progesterone challenge.
48
Leuprolide,nafarelin,histrelin -use
GnRH agonist -Pulsatile-->agonist Continues-->first agonist,later antagonist -ER+ Breast cancer, Prostate cancer,Endometriosis,Fibrinoids,Pre-cocious puberty---> Continous fashion -Infertility-->pulsatile
49
Dagirelix Why is it better than other medications used?
GnRH recep antagonist-->acts via Gq (decr IP3) -Prostate cancer. **-NO start up flare**
50
2 Contraceptive mechanism and thir action Adverse effects
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
Abortificant medication -Use with what medication.
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
Treat for PCOS (6) -Why do you want this patients to go throught weight loss and treat them with OCP?
**-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
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).
54
Side effects of Danazol?
-Intra-cranial Hypertension,Edema,Maculanization

ENDO/REPRO (10 decks)

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