hormones Flashcards
4 types of hormone therapies
Thyroid Disease
Menopausal Hormone Therapy
Contraception
Selective Estrogen Receptor Modulators (SERMs)
what does the thyroid gland do?
The thyroid gland, albeit non-essential for life, governs tissue metabolism
how is normal growth and maturation made possible?
Normal growth and maturation is made possible by maintaining an optimal level of tissue metabolism
what are T3 and T4? What do they stand for? Which is most active?
Triiodothyronine (T3; most active) and thyroxine (T4) are two major thyroid hormones
what 3 things does hypothyroidism cause?
Hypothyroidism causes bradycardia, poor cold resistance, and mental/physical slowing
what 5 things does hyperthyroidism cause?
Hyperthyroidism causes tachycardia, body wasting, tremor, nervousness, and heat flashes
2 drugs for hypothyroidism?
Levothyroxine [Synthroid®, Levoxyl®]
Liothyronine [Cytomel®]
2 drugs of hyperthyroidism?
Propylthiouracil (PTU)
Methimazole [Tapazole®]
whats the number 2 highest selling drug in america?
levothyroxine sodium
indication for levothyroxine
INDICATION
Hypothyroidism
DOSING [50-200ug]
1 tab qd
moa of levothyroxine soidum?
CLINICAL PHARMACOLOGY
Thyroid hormone replacement
Mechanism of Action
Synthetic T4 (tetra-iodothyronine)
adverse effects of levothyroxine sodium
ADVERSE EFFECTS
Common: Weight loss, diaphoresis, headache, alopecia
CV: Hypertension
CNS: Pseudotumor cerebri (children), hallucination [ψ]
OCULAR: Ptosis, diplopia, EOM paresis
levothyroxine sodium drug interactions
DRUG INTERACTIONS
Sympathomimetics (Additive)
what 3 things characterize menopause?
Menopause is characterized by reduced libido, vasomotor instability (hot flashes) and vaginal atrophy
estrogen dosing for menopause compared to contraception
Estrogen dosing for menopause is significantly lower and therefore safer than for contraception
what the most potent estrogen produced and secreted by the ovary?
estradiol
what is a metabolite of estradiol w/ 1/3 potency, which is the primary circulating estrogen after menopause
estrone
because estrogens have a chloesterol back bone, what are they able to do?
Having a cholesterol backbone, estrogens dissociate from their globulin or albumin binding sites and readily cross cell membranes to bind to nuclear receptors where they affect gene transcription and translation
3 menopausal therapies
Estrone [Menest®]
Estradiol
Mestranol [Necon®]
estrone indication
INDICATION
Menopause, Breast Cancer, Prostate Cancer, Osteoporosis prevention
DOSING [0.3-2.5mg]
1 tab PO qd
CLINICAL PHARMACOLOGY
Hormone Replacement Therapy (HRT)
Mechanism of Action
Binds to estrogen receptors, developing and maintaining female sex characteristics and reproductive systems
moa of estrone
ADVERSE EFFECTS
Common: Headache/migraine, elevated BP, weight changes, fluid retention, contact lens intolerance, vision changes
SEVERE ADVERSE EFFECTS
BLACK BOX: Endometrial Cancer, Stroke, DVT, MI, Invasive Breast Cancer
adverse effects of estrone
estrone drug interactions
DRUG INTERACTIONS
Azole Antifungals (Impaired metabolism)
Adverse effects of systemic steroids may be increased
Anti-hyperlipidemic effects of Omega-3 FA’s may be antagonized
CONTRAINDICATIONS
Hypertension
Smoker
Migraine [with aura] > [without aura]
estrone contraindications
contraception drug
Drospirenone/Ethinyl Estradiol [Yaz®]
ways contraceptive agents are grouped
monophasic, biphasic, triphasic, and four phasic vs progestin only
indication for yaz
INDICATION
Contraception, Acne Vulgaris, Dysmenorrhea, Endometriosis, PCOS
DOSING [3 mg/20 ug]
1 tab PO qd
moa for yaz
CLINICAL PHARMACOLOGY
Hormone Therapy
Mechanism of Action
Suppresses LH and FSH, inhibiting ovulation; alters cervical mucus and endometrium
yaz adverse effects
ADVERSE EFFECTS Common: Headache, weight changes, BP elevated, increased cholesterol, contact lens intolerance SEVERE ADVERSE EFFECTS MI, stroke, ocular lesions BLACK BOX Smoking and CV Events
yaz drug interactions
DRUG INTERACTIONS Impaired metabolism of Cyclosporine NSAIDs (Additive hyperkalemia) Tetracyclines, Penicillins, Cephalosporins, Macrolides, Quinolones (Decreased efficacy) Ascorbic Acid (Decreased metabolism)
yaz contraindications
CONTRAINDICATIONS
Hypertension
Smoker
Migraine w/ aura > w/o aura
selectivity property of SERMs refers to what?
their ability to inhibit or stimulate estrogen receptors depending on the tissue
uses of SERMs include what?
Uses include management of breast cancer, osteoporosis, menopause and anovulation
3 types of SERMS
Tamoxifen [Soltamox®]
Clomiphene [Serophene®, Clomid®]
Raloxifene [Evista®]
INDICATION for tamoxifen
INDICATION
Metastatic Breast Cancer
DOSING [10/20 mg]
1-2 tabs qd-bid
moa of tamoxifen
CLINICAL PHARMACOLOGY
SERM
Mechanism of Action
Binds to estrogen receptors, producing estrogenic and anti-estrogenic effects
adverse effects of tamoxifen
ADVERSE EFFECTS Common: Dizziness, headache, VA changes SEVERE ADVERSE EFFECTS Thromboembolism, stroke Pancytopenia Retinopathy, cataracts
drug interactions of tamoxifen
TAMOXIFEN
DRUG INTERACTIONS
May increase Cyclosporine, Systemic Steroid, Oxycodone levels
Chlorpheniramine, Macrolides (Inhibit hepatic production of active metabolite)
