Pharm endocrine (hypothalamus/pit) Drugs Flashcards
1
Q
Somatropin (ant. Pit) - GH+
A
- MOA:
- Recomb forms of Human growth hormone
- Acts GH receptors to increase IGF-1 (liver)
- Net Effect:
- Promotes protein deposition (lean body mass)
- Enhances fat use
- Decrease carb use
- Stimulates growth of cartilage & bone
- Pharmokinetics(body does to drug):
- Subcutneous admin (1/2 life short) 6-7x a week
- Therapy stopped until adequate height reached, epiphyses close or reponse stops
2
Q
Somatropin (ant. Pit) - GH+
A
- Clinical Use: (Replacement therapy)
- Replace in GH def - Turner’s syndrome, prader-willi, chronic kidney disease
- Adverse effects:
- More prominent in adults
- Scoliosis, edema, gynecomastia(benign growth of breast tissue), intracranial hypertension, carpal tunnel, Increased CYP450 activity
- Contraindications:
- Closed epiphysis, underlying intracranial lesion, active malignancy, diabetic retinopathy
3
Q
Pegvisomant (ant. pit) - GH(-)
A
- MOA:
- Blocks GH receptors = GH antagonist
- PK:
- Daily subcutaneous admin
- Clinical applications:
- Acromegaly - Or for pts who are NOT responsive to somatostatin analogs (natural inhibitor of GH)
- Adverse effects:
- Elevated liver enzymes
- Hypertension, peripheral edema, Paresthesias (tingling), dizziness
- Due to 2x GH
- MRI to check on enlarging adenoma
4
Q
Mecasermin (ant.pit) - IGF +
A
- MOA:
- Recombo form of IGF-1 stims IGF-1 receptors
- PK:
- SC injection 2x/daily Given right after snack
- Clinical uses:
- Laron dwarfism (insensitive to GH)
- GH-def w/neutralizing antibodies
- IGF-1 def that is NOT responsive to GH
- Adverse effects:
- Hypoglycemia, intracranial hypertension, INCREASED liver enzymes
- Contraindicated: in pts w/closed epiphyses or with suspected active neoplasm (tumor)
5
Q
Sermorelin (GHRH)-hypothalamus
A
- Shortest Pharm active analogue
- Used in diagnostic purposes
- Specific drug (orphan) = GH def & weight loss in Aids pts
- Used in athletic doping & youthful rejuvenation spas
6
Q
Octreotide (hypothalamus)
A
- Somatostatin VERY short 1/2 life 1-3 minutes - used for theraputic purpose
- MOA:
- Somatostatin receptor agonist +
- Clinical uses:
- Acromegaly
- Diarrhea from carcinoid tumors (GI)
- TSH-producing adenomas
- Diarrhea from vasoactive GI-peptide secreting tumors
- PK:
- 45 X more potent than somatostatin
- 1/2 life 80 min
- SC 3xday or IM 1x day
- Adverse effects:
- Ab pain, constipation, nausea, arrythmias, bradycardia, hypoglycemia, gallstones
7
Q
Gonadorelin (Hypothalamus)
A
- GnRH analogue
- Clinical uses:
- Diagnosis of hypogonadism
- stimulate ovulation (pulsatile form)
- Adverse effects:
- Anaphylaxis w/multiple doses
- Headache, flushin, lightheaded
8
Q
Leuprolide (Hypothalamus) GnRH +
A
- MOA: GnRH agonist +
- PK:
- IV, SC, IM or intranasaly (nafarelin)
- Depot forms = decrease gonadal steroid production
- Clinical uses:
- Ovarian suppression (ovarian hyperstim)
- Endometriosis, uterine fibroids
- Porphyria (skin & blood)
- Percocious puberty (early puberty)
- Advanced breat/prostate cancer (androgen dependent)
- Adverse effects:
- Hot flashes, Gynecomastia (irreversible), osteoporosis, sex dysfunction
- DVT w/Goserelin & leuprolide
9
Q
Ovulation Induction
A
- Major side effects:
- multiple pregers
- Ovarian hyperstim syndrome (direct use of drugs) = enlarged ovary, ascites, shock
- 3 steps to induction:
- Inhibit endogenous gonadotropin production - using GnRH agonist (continuous) or antagonist
- Induce follicle development: Daily injections menotropins, FSH or analogue
- Induce oocyte maturation: LH or analogue injection, OR use GnRH agonist (less risk for OHSS)
10
Q
Ganirelix (hypothalamus) GnRH(-)
A
- MOA:
- Antagonist of GnRH receptors (-)
- PK: SC injections
- Clinical uses:
- Prevention of premature LH surges during controlled ovulation hyperstimulation
- Adverse effects:
- Headache, nausea
- OHSS
- Ectopic pregnancy, Thrombotic disorder, spontaneous abortion
11
Q
Cetrolix (hypothalamus) GnRH(-)
A
- NOT 1st line - potential for anaphylaxis
- Clinical uses:
- Controlled ovarian hyperstimulation
- hormone sensitive breast/prostate cancer
- endometriosis
- Degarelix - used only in ADVANCED prostate cancer
12
Q
Follitropin (rFSH) & Urofollitropin (FSH)
A
- MOA:
- Stimulate gonadal maturation & steroid production
- Clinical uses:
- Ovulation induction
- Male hypogonadotropic hypogonadism (GIVEN with Human chorionic gonad)
- Adverse effects:
- Multiple fetuses
- Ovarian cysts (hypertrophy)
- Upper resp infections
- Embolism & thrombosis
- OHSS
13
Q
Male hypogonadotropic hypogonadism
A
- Causes:
- Kallman syndrome (anosmia - inability to smell)
- Inflammatory disease
- HIV/AIDS
- Pituitary tumor
- Obesity
- Opiates
14
Q
hCG (LH receptor +)
A
- Types: Choriogonadotropin alfa (hCG), Lutropin alfo (form of LH)
- Menotropins (hMG) - extract of urine from postmenopausal women (FSH & LH)
- Clinical uses:
- Starting ovulation during controlled ovulation hyperstim
- Ovarian follicle development in women with hypogonadotropic hyogonadism
- And in MALES combo with FSH
- MOA: Agonist of LH receptor
- PK: IM injection 2-3x week
- Adverse effects:
- Headache, depression, edema
- OHSS in women and gynecomastia in men
15
Q
Bromocriptine (hypothalamus)
A
- Treatment: reduces prolactin & higher doses reduce GH
- MOA: Dopamine analog
- agonist @ dopamine receptors (D2)
- Other clinical uses:
- Parkinson’s (combo with L-dopa) -linked to valvular heart disease due to HIGH doses
- NOT to be used in women to stop lactation following stillbirth
- PK: Oral or vaginal admin (large oral dose absorbed in liver)
- Adverse effects:
- GI
- Orthostatic hypertension
- Psychiatric disturbance
- Cabergoline: similar effects (LESS GI)
