A: 6-11 Flashcards
What is the drug of choice if we want to replace Cortisol?
Hydrocortisone
כמו שצריך היידריישן אם חסר לך מים
Which corticosteroid has a short duration of action?
Hydrocortisone
8-12 h
אתה כל הזמן צריך לשתות מים זה לא מספיק פעם אחת
Which cortico. has intermediate duration of action?
Triamcinolone
Prednisolone
Methylprednisolone
Which cortico. has a long DOA?
Dexamethasone
36-72 h
Prednisolone and Methylprednisolone indications
Systemic anti-inflammatory and immunosuppressive effects
Triamcinolone indication
Topical
T=T
Which cortic. has an increased toxicity?
Triamcinolone
Toxic=T
Dexamethasone indication
Antiinflammatory
Immunosuppressive
Used when water retention is undesirable
How do cortico. present in the body?
90% bound to CBG
5-10% free form
Cortico. metabolism
80% hepatic
20% renal
Cortico. immunologic MOA (8)
Lower Leuko. migration Lower capillary permeability PLA2 inhibitionn Lower COX-2 expression Lower PLT activator factor Lower IL Inhibits NF-kB Apoptosis of Lymphocytes
Glucocort. for topical use
Budesonide
Fluocinolone
Fluticasone
Mometasone
BFF Me!!!
Topical glococort. indications
Asthma Dermatology Allergic rhinitis Conjunctvitis Arthritis IBD's
Which drug blocks 11B-Hydroxylase?
Metyrapone
מתיר אפון
Mineralocorticosteroids: (2)
+ Duration of action
Aldosterone 1-2 h
Fludrocortisone 8-12 h
What is the drug of choice for replacement therapy of Aldosterone?
Fludrocortisone
Mineralcort. side effects
Slat and water retention HTN CHF Cardiac remodeling Glucocort. excess
What are the synthestic analoges of Testosterone?
How to take?
Testosterone undecanoate- orally
Nandrolone- Parenteral
What counts as an anabolic testosterone steroid?
Nandrolone
קצת כמו נאנדתרל
Synthetic Testosterones indications
Hypogonadism in boys
HRT
Stimulates RBC production in some anemias
Female side effects of Testosterone?
Virilization
Menstrual irregularuty
Male side effects of Testosterone
Feminization due to feedback mechanism
Prostate pathology
Both sexes side effects of Testosterone
Cholesthatic jaundice
Increased liver enzymes
Hepatocellular carcinoma
Testosterone contraindication
Pregnancy
Prostate cancer
CHF
Liver disease
Antiandrogens can be divided into
Receptor inhibitiors: Bicalutamide
5a-reductase inhibitors: Finasteride
GnRH agonist: Gosereline
GnRH antagonists: Degarelix
Bicalutamibe MOA
Competative inhibitor of androgen receptor
Bicalutamide indications (2)
Prostate cancer
Precocious puberty
Bicalutamide side effects
Gynecomastia
Flushes
Impotence
Hepatotoxicity
Which enzyme catalize the convertion of Testosterone into DHT
5a-reductase
Which drug is a 5a-reductase inhibitor?
Finasteride
Finasteride indications
BPH
Can prevent male baldness
GnRH agonist
Goserelin
What is the long term effect of Goserelin?
Suppression of gonadotropin secretion
Gosrerlin indication
Central precocious puberty
Prostate cancer
Degarelix MOA
GnRH antagonist
Drug that affect sexual activity
Sidenafil
Sidenafil MOA
PDE-5 inhibitor
PDE-5 job
breaks down cGMP –> Vasoconstriction
PDE-5 inhibitors MOA
cGMP increases –> Vasodilation
PDE-5 inhibitors route
Oral
Commercial name of Sildenafil
Viagra
Sildenafil indications
Erectile dysfunction
Pulmonary HTN
BPH
Give an example for synthetic Estrogen
Ethinyl-Estradiol
Ethinyl Estradiol metabolism
CYP 450
Ethinyl-Estradiol indications
Hypogonadism
HRT
Prevent bone loss
Contraceptive
Which Estrogen drug can be given to treat menopause symp.?
Estradiol
Estrogen side effects
Moderate toxicity
Bleeding
Nausea
Breast tenderness
Estrogen side effects
Severe toxicity
Thromboembolism Gallbladder Hyper TG Migrane HTN Depression
Selective Estrogen Receptor Modulators (3)
Raloxifen
Clomifen
Tamoxifen
R-CT
SERM- what is it selective for?
Antagonist at breast, CNS, uterus
Agonist at liver and bone
Tamoxifen indication
Hormone responsive breast cancer
Tamoxifen side effects
Hot flushes
Thromboembolism
Endometrial hyperplasia
Raloxifene indications
Prevention of osteoporosis in postmena.
Clomifene indications
Ovulation induction
SERM drugs are given through
Oral
Clomifene MOA
Selective inhibition of Estrogen-R in pituitary –> Reduced NF –> Induce LH/FSH secretion
Aromatase inhibitor
Anastrozole
אנס את הארומטייז
Anastrozole indications
Adjuvent treatment of hormone responsive breast cancer
אנס את הסרטן
Anastrozole side effects
Flushes
Bone density down
Joint symp.
What is Gosereline MOA?
Synthetic peptide with GnRH agonist activity
Goserelin indications in females
Overian suppression in Endometriosis and Leiomyoma
Central precocious puberty
Degarelix MOA
GnRH antag.
Degarelix female indication
Controlled ovarian stimulation
Describe Progestin
Induce secretory change in the endometrium
Breast proliferation
Maintenance of pregnancy
Metabolic effect
Synthetic Progestrones (6)
Medroxy.progesterone Nor.ethi.sterone- הציפורים עפות צפונה Cyproterone acetate- ציפור טרון Dro.spire.none - דרור ספיר Desogestrel Levo.nor.gestrel
Synthestic Progesterone indications
HRT Contraceptive Infertility Prevent endometrial cancer (Estrogen-induced) Promote and maintain pregnancy
Synth. Progest. metabolism
CYP 450
Progestins side effects (6)
Lowers HDL Increases LDL HTN Weight gain Decreases bone density Increases breast cancer risk
Anti Progestins
Mifepristone
Ulipristal acetate
UMMM i dont want to be pregnant
מי פה הפריסט?
אולי הפריסט יעשה לי הפלה?
Mifepristone MOA
Progestin and Glucocort. R antagonist
Mifepristone indications
Meidcal abortion up to 49 days after last menstrual
Mifepristone side effects
GI
Vaginal bleeding
Atypical infections
Ulipristal acetate MOA
SPRM
Ulipristal acetate indications
Emergancy birth pill
Myoma growth suppression
Hormonal contraceptive- preparation available (6)
Pill Transdermal patch: 1 week Vaginal ring: 3 weeks Injection: 8 weeks IUD: 5 years SC implants: 3-6 years
Types of preparation used for oral contraceptive (2)
Combination of Estrogen and Preogestin
Contineous Progesterin therapy without Estrogen
Biphasic contraceptive which are the agents?
Ethinyl-Estradiol (Always)
Levonorgestrel or Desogestrel
Oral contraceptive MOA
Combination of Estrogen and Progestin –> selectively inhibits the pituitary from releasing LH/FSH –> NO LH surge –> no ovulation
oral contraceptive side effects
MILD(5)
GI Edema Endocrine Headache Withdrawal bleeding
Moderate oral contraceptive side effects (7)
Weight gain Skin pigmentation Acne Hirsutism Ureteral dilation Vaginal infections Amenorrhea
Severe oral contraceptive side effects
Thromboembolism
GI
Depression
Oral contraceptive contraindiccation
Recurrent thromboembolic/cardiovascular events Estrogen neoplasms Vaginal bleeding Prior to epiphyseal closure Smoking
Emergency contreceptive contains
High dose Progesterin- Levonorgestrel
Or Ulipristal acetate
Progesterone derivative that is more resistant to metabolism for improved pharmacokinetic properties
Medroxyprogesterone-acetate
MPA