Term
| Name the hypothalamic hormones |
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Definition
•GHRH
•Somatostatin
•Thyrotropin releasing hormone (TRH)
•Corticotropin releasing hormone (CRH)
•GnRH
•Dopamine (PIH)
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Term
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Definition
•Found in pancreas and CNS
•Inhibits release of GH, thyrotropin, glucagon, insulin and gastrin
•Inhibits the release of gut peptides including VIP (vasoactive intestionalomas)
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Term
Name the somatostatin analogue
Use?
ADR? |
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Definition
Octreotide: synthetic octapeptide somatostatin analog (long duration of action)
Used in tx of:
–Acromegaly
–Carcinoid syndrome (serotonin 5-HT - biomarker)
–Gastrinoma, VIPoma
–Esophageal varices related bleeding
ADR: Gall stone formation
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Term
GnRH analogs.
ROA & why this is important?
Uses |
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Definition
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•Pulsatile administration is used to stimulate the release of FSH and LH from the anterior pituitary - pituitary and gonadotropin stimulation in infertility
•In contrast, long term (2 to 4 weeks) administration leads to decreased FSH and LH secretion, after initially stimulation –Chemical castration: useful in hormone dependent tumors (prostrate, breast), endometriosis and fibrioids
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Term
Name the GnRH agonist drugs
Use? |
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Definition
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GnRH agonist preparations
•Gonadorelin – short acting
•Leuprolide (CA prostate), Nafarelin, Buserelin, Goserelin – long acting
Prostate cancer & Male baldness
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Term
Name the GnRH antagonist drugs
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Definition
GnRH antagonist preparation:
•They are pure antagonists and do NOT cause initial surge of FSH and LH
•Ganirelix
•Cetrorelix
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Term
| What are the other uses of GnRH agonists? |
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Definition
GnRH agonists are used to suppress gonadotropin
secretion (in steady dosage) in patients with:
–Prostatic carcinoma
–Endometriosis
–Precocious puberty (early puberty)
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Term
| Which 2 hormones are released from a different area? |
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Definition
Oxytocin (uterine muscles & mammory glands)
ADH/ vasopressin (kidney)
- supraoptic & paraventricular nucleus of the hypothalamus - transported to the posterior pituitary for release |
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Term
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Definition
Somatotrophin - growth hormone
FSH - Oestrogen
LH - Progesterone |
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Term
What are the drugs used as GH analogs?
Use?
ADR? |
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Definition
•Somatropin (Humatrope)
Somatrem (Protropin)
GH deficiency, chronic renal failure, turner’s syndrome & Wasting in patients with HIV/AIDS.
A/E : includes edema (due to increase Na retention), carpal tunnel syndrome, rarely ↑ ICT
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Term
What is Laron syndrome?
What is used to treat it?
MOA? |
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Definition
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Laron syndrome, or Laron-type dwarfism, is an autosomal recessive disorder characterized by an insensitivity to growth hormone (GH).
•IGF-1 preparation: Mecasermin
•It is recombinant IGF-1 and an effective treatment for GH insensitive patients also approved for GH deficiency.
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Term
What are the symptoms of Acromegaly?
What is used to treat it?
MOA? |
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Definition
| acromegaly - characterised by acralenlargement and soft tissue overgrowth of the hands and feet, coarsening of facial features and thickening of the skin. •Pegvisomant – (Somavert): a new GH receptor antagonist. |
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Term
Patient was given treatment for growth, resulting in dementia, tremors and lack of motor co-ordination.
What is the disorder?
What was the patient given?
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Definition
Creutzfeldt-Jakob disease (CJD)
It resulted because of human cadaver GH preparations. |
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Term
What is the precursor for ACTH & MSH?
What is the role of ACTH? |
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Definition
Proopiomelanocortin (POMC)
stimulate the zona faciculata and zona reticularis to produce the cortisol and adrenal androgens. |
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Term
What are the ACTH analogs?
ADR's? |
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Definition
•Corticotropin - porcine ACTH.
•Cosyntropin - synthetic form of human ACTH.
•ADR: Acne, hirsutism**
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Term
| What is another use of Cosyntropin |
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Definition
•Cosyntropin - is employed in diagnostic test to diagnose congenital adrenal hyperplasia.
•To diagnose adrenal insufficiency in a test that measures cortisol before and after cosyntropin injection
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Term
Name the gonadotropins
Action |
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Definition
FSH -
Females - Folicle stimulation & release of oestrogen
Males - Spermatogenesis
LH -
Females - stimulates ovulation
Males - testosterone release |
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Term
Name the Gonadotropin analogues
Uses? |
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Definition
•Urofollitropin / Follitropin is a FSH agonist.
•Menotropins contains FSH and LH.
•Human Chorionic Gonadotropin is a LH agonist
–Used to treat un-descended testis – aka criptorchism (if no anatomical blockade)
Uses:
•To induce ovulation
•Infertility in men and women
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Term
Prolactin Release Inhibitory Hormone
AKA?
Use?
If there is a Defect what happens?
How is this treated? |
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Definition
Dopamine which inhibits the release of prolactin
Hyperprolactinemia, galactorrhea & infertility - treat with D2 agonist - Bromocriptine or CABERGOLINE |
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Term
What is used in the treatment of preterm labour
MOA? |
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Definition
ATOSIBAN - oxytocin antagonist
- during late pregnancy the uterus becomes very sensitive to oxytocin due to an up-regulation of receptors, this causes the uterine muscle to contract, which is not beneficial in pre term labour, thus an oxytocin antagonist is given.
Can also give - B2 agonist, Ca channel blocker |
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Term
What is used to induce labour?
What are other uses of this analog?
What are the ADR's
When is it contraindicated? |
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Definition
•Synthetic oxytocin used to induce uterine contractions during labor.
•It is also used to prevent postpartum uterine hemorrhage. (DOC: ergots**)
•A nasal preparation is available for milk let down reflex in nursing mothers.
•ADR's - Seizures, hypotension and hyponatremia are usual adverse effects.
•It is contraindicated in fetal distress, cephalopelvic disproportion
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Term
What is the DOC for post partum hemmorhage?
MOA?
What can also be used? |
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Definition
Ergonovine - Given IM in Postpartum hemorrhage and Placental retention
MOA: Acts through Alpha or serotonin receptors
Oxytocin agonist
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Term
When is ADH or Vasopressin released?
Where does it act? |
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Definition
In response to a low ECF volume, i.e Hypotension, hypovolemia, hyperosmolarity
V1 - Blood vessels - Vasoconstriction
V2 - Collecting duct - Fluid retention
Both leading to an increased BP |
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Term
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Definition
****Diabetes insipidus (neurogenic)
Nocturia
Bleeding oesophageal varices
Haemophilia A (increases factor VIII)
vonWillbrand’s disease (increases vW factor)
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Term
| Name the natural oestrogen's |
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Definition
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Estradiol,
Estrone
Estriol.
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Term
| Name the synthetic steroidal estrogens |
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Definition
Ethinyl Estradiol,
Mestranol.
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Term
| Name the synthetic non steroidal estrogens |
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Definition
Diethylstilbestrol,
Dienestrol |
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Term
| What are the Uses of Oestrogen's? |
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Definition
•Hypogonadism in girls.
•Hormonal replacement therapy
•Contraception
•Osteoporosis
•Prostate carcinoma
•Turner's syndrome (Gonadal dysgenesis).
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Term
| What are the ADR's associated with Oestrogen? |
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Definition
↑ risk of myocardial infarction, stroke,
gall stones and pulmonary embolism - due to the increase in factor II, VII, IX, X, fibrinogen and ↓ anti-thrombin
Mastalgia (pain in breast)
↑ the risk of endometrial and breast cancer.
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Term
What is a specific use of diethylstilbestrol (DES).
What is a specific ADR of DES?
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Definition
DES is still one of the most commonly used agents for the hormonal treatment of advanced prostate cancer - via negative feedback decreasing LH levels
DES during breast feeding increase vaginal adenocarcinoma in female offspring.
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Term
Estrogen antagonist
Drug?
Use?
MOA? |
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Definition
Clomiphene
Used as ovulation inducing drug for patients who have cycles where oocyte is not released
Acts as a competitive inhibitor at estrogen receptor - It decrease the negative feedback of estrogen on hypothalamus / pituitary and increase FSH / LH secretion.
A/E– multiple pregnancy and ovarian enlargement.
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Term
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Definition
•First generation: Norethindrone, Ethynodiol diacetate.
•Second generation: Levonorgestrel, Norgestrel.
•Third generation: Desogestrel, Norgestimate.
•Fourth generation:Drospirenone.
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Term
What are the clinical uses of the progestins?
ADR's? |
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Definition
-HRT - to counteract the endometrial hyperplasia seen with Oestrogen
-Contraception
•Breakthrough bleeding,
Hirsuitism and acne (androgenic)
•Abnormal lipid and glucose levels.
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Term
Antiprogestin
Drug?
MOA?
Use? |
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Definition
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Mifepristone:
•It is a progesterone receptor antagonist. It is also a glucocorticoid receptor antagonist.
•If mifepristone is taken shortly after intercourse, it prevents pregnancy.
•Mifepristone (in combination with miopristol) widely used to terminate early pregnancy.
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Term
Oral contraceptives
Types?
MOA? |
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Definition
1.Estrogen and Progestin
2.Progestin Only
These exert the contraceptive effect mainly
through selective inhibition of gonadotropin
release from the pituitary, especially
midcycle LH surge (which initiates ovulation)
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Term
| Name the constituents of Oral contraceptives |
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Definition
•Estrogen:
Ethinly estradiol (EE),
Mestranol
•Progesterone:
Norethindrone,
Norgestrel,
Levonorgestrel,
Desogestrel,
Drospirenone
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Term
| What is the difference between Monophasic, triphasic & diphasic hormoal contraceptives |
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Definition
Biphasic - contains the same amount of progesterone & estrogen throughout the cycle
Triphasic & Diphasic - contain a variable amount of Estrogen & Progesterone over the cycle |
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Term
| What are the Postcoital contraceptives? |
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Definition
•Oral levonorgestrel: within 120 hours for best results.
•Estrogens & Progestins : It is started within 72 hrs for best results.
•Mifepristone is effective as postcoital contraception along with misopristol (PGE1) .
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Term
| Where is testosterone produced? |
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Definition
95% in the Leydig cells of the testies
5% in the adrenal gland |
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Term
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Definition
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Synthetic Androgens : It is a weak androgen, derivative of testosterone which has anti-estrogenic activity.
•Primarily used in endometriosis and fibrocystic breast disease.
•It is also used in the treatment of hereditary angioedema (↑C-1 esterase inhibitor).
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Term
Testosterone
ROA
Specific Drugs and their ROA |
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Definition
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•It is given i.m or transdermally to avoid extensive hepatic metabolism.
•Testosterone cypionate is available for intramuscular administration.
•Methyltestosterone is active orally and resistant to hepatic metabolism, but can result in hepatoxicity.
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Term
Name the progesterone only mini pills
ROA?
duration of action?
Use? |
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Definition
•Norethindrone (Nor-QD): oral admin.
•Levonorgesterol: implanted under the skin - effective for 5 years
•Medroxyprogesterone depot injection - 3 months
Suited for smoker, breast feeding and estrogen intolerance |
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Term
Name the synthetic androgens
Clinical use?
ADR?
Contraindications? |
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Definition
Oxandrolone
Nandrolone
Clinical uses :
Hypogonadism, Endometriosis, Anemia, Osteoporosis, Aging. Illicit use in athletics**
Adverse effects :
Hirsutism, acne, deepening of voice.
Cholestatic jaundice.
Contraindications: Pregnancy & Prostate cancer.
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Term
Finasteride
MOA?
Use?
ADR? |
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Definition
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•Orally active and inhibits 5-α-reductase -II enzyme which converts testosterone to dihydrotestosterone - producing a reduction of dihydrotestosterone in prostate and skin.
•It is approved for treatment of benign hypertrophy of prostate.
Loss of labido, erectile dysfuncion
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Term
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Definition
Androgen blocker
Ca of prostate |
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Term
What is the best combination therapy used in BPH?
Why? |
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Definition
Alpha 1 blocker & 5-alpha reductase inhibitror
-it reduces all the symptoms i.e urinary retention, urinary insufficiency etc. |
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