Block 1 Endocrine pharmacology Flashcards
Describe the MOA of Raloxifine
It’s a selective estrogen receptor modulator which acts a:
- An antagonist at the breast & uterus
- An partial agonist at the bone
What are the side effects of Raloxafine?
Increased risk of thromboembolic events (DVT & PE)
Which one causes endometrial cancer? Raloxifene or Tamoxifen?
Tamoxifen
What are the clinical uses of Raloxifene?
Osteoporosis in post menopausal women
&
Breast cancer prophylaxis
Osteoporosis in post menopausal women
&
Breast cancer prophylaxis
Are clinical uses of which drug
Raloxifene
Describe the MOA of Tamoxifen
It’s a selective estrogen receptor modulator which acts a:
- An agonist in the bone & uterus
- antagonist in the breast
What are the side effects of Tamoxifen (9)
- Higher risk of thromboembolism (esp in smokers)
- Endometrial cancer
- Hot flashes
- Nausea/vomiting
- Menstrual irregularities
- Post menopausal bleeding
- Vaginal discharge
- Pruritis vulvae
- Dermatitis
- Higher risk of thromboembolism (esp in smokers)
- Endometrial cancer
- Hot flashes
- Nausea/vomiting
- Menstrual irregularities
- Post menopausal bleeding
- Vaginal discharge
- Pruritis vulvae
- Dermatitis
Are all side effects of which endocrine drug?
Tamoxifen
What are the clinical uses of Tamoxifen?
Treat & prevent the reoccurrence of ER/PR +ve breast cancers
What drug can be used to Treat & prevent the reoccurrence of ER/PR +ve breast cancers
Tamoxifen
Describe the MOA of Bisphosphonate (dronates)
They are analogs of pyrophosphate, so they can stabilize the hydroxyapatite bone structure
&
It also induces osteoblasts to secrete more osteoclastic inhibitors (reduce bone reabsorption)
What are the clinical uses of Bisphosphonates?
- Osteoporosis in post menopausal women
- Paget’s disease
- Hypercalcemia of malignancy
- Osteolytic bone metastases
- Osteoporosis in post menopausal women
- Paget’s disease
- Hypercalcemia of malignancy
- Osteolytic bone metastases
Can all be treated by which endocrine-specific drug?
Bisphosphonate
phospho pulls Ca2+ into bone
What are the side effects of Bisphosphonates?
Bone mineralization
GI diseases (esophageal ulcers)
Osteonecrosis
Bone mineralization
GI diseases (esophageal ulcers)
Osteonecrosis
Can be caused by which endocrine-specific drug?
Bisphosphonate
Describe the MOA of Aromatase inhibitors
They inhibit the peripheral conversion of androgens into estrogen (lower estrogen levels)
What are the clinical uses of Aromatase inhibitors?
Treat ER+ve breast cancer in post menopausal women who are resistant to Tamoxifen
Which drug would you use to treat ER +ve Breast cancer in postmenopausal women who are resistant to Tamoxifen?
Aromatase inhibitor
Letrozole, Anastrozole, & Exemestane are all examples of which type of drug class?
Aromatase inhibitors
What are the side effects of Aromatase inhibitors?
- Accelerated bone loss
- Osteoporosis
- Fractures - Arthritic symptoms
- Hot flushes (nausea/diarrhea)
AA
- Accelerated bone loss
- Osteoporosis
- Fractures - Arthritic symptoms
- Hot flushes (nausea/diarrhea)
Are side effects of which endocrine-specific drug?
Aromatase inhibitor
Describe the MOA of HRT’s
They increase estrogen & reduce osteoclastic activity (reduce bone loss)
What are the side effects of HRT when unopposed estrogen replacement is used?
Higher risk of;
Endometrial cancer
Cardiovascular disease
When unopposed estrogen replacement is used (HRT), what can be used to reduce the risk of Endometrial cancer?
Progesterone & progestin to avoid this
What are the clinical uses of HRT?
Relief or prevention of menopausal symptoms & osteoporosis
Describe the MOA of Glucocorticoids
They interact on specific receptors within target tissues to regulate their expression of corticosteroid-responsive genes which can either increase/or/decrease the expression of these genes to control the synthesis of inflammatory mediators
What are the side effects of glucocorticoids?
Cushing’s
Osteoporosis
Retarded growth (muscle atrophy)
Thin skin
Immunosuppression
Cataracts/gluacoma
Osteonecrosis
Suppression of HPA-axis
Teratogenic effects
Emotional disturbances (depression)
Rising BP
Obesity (truncal)
Increased hair (Hirsutism)
Diabetes Mellitus
Striae
CORTICOSTEROIDS
Cataracts
Cushings
Diabetes mellitus
Edema
Glaucoma
Muscle atrophy (limbs)
Osteoporosis
Osteonecrosis
Peptic ulcer disease
Risk of infection
Suppression of HPA-axis
Are all side effects of which endocrine-specific drug?
Corticosteroids
Describe the MOA of mineralocorticoids
They bind to cytoplasmic receptors & can effect gene transcription
What are the side effects of Mineralocorticoids
Cataracts
Cushings
Diabetes mellitus
Edema
Glaucoma
Muscle atrophy (limbs)
Osteoporosis
Osteonecrosis
Peptic ulcer disease
Risk of infection
Suppression of HPA-axis
&
EDEMA
WORSE CARDIAC CONDITION
Describe the MOA of the anabolic steroid Methyltestosterone
It acts as an agonist at the androgen receptors to activate them
What are the side effects of Methyltestosterone?
- Excessive masculinization
- Premature closure of the epiphysis
- Cholestatic jaundice
- Dependence
- Acne
- Gonadal atrophy
- Decreased intratesticular testosterone
- Dyslipidemia (high LDL & low HDL)
- Excessive masculinization
- Premature closure of the epiphysis
- Cholestatic jaundice
- Dependence
- Acne
- Gonadal atrophy
- Decreased intratesticular testosterone
- Dyslipidemia (high LDL & low HDL)
Are all symptoms of which anabolic steroid?
Methyltestosterone
Describe the clinical uses of Methyltestosterone
- Male hypogonadism
- Anabolic actions (increase muscle mass, high RBC, & low nitrogen)
- Precocious puberty in males
- Male hypogonadism
- Anabolic actions (increase muscle mass, high RBC, & low nitrogen)
- Precocious puberty in males
Are all conditions that can be treated with which anabolic steroid?
Methyltestosterone
Describe the MOA of Hormonal contraceptives
They suppress LH & FSH which causes an absent mid-cycle surge of LH that causes a decrease in endogenous steroid levels thereby inhibiting ovulation
What are the side effects of oral contraception?
- Thromboembolism
- Pulmonary embolism
- Stroke
- Hypertension
- Genital carcinomas
- Gall bladder disease
- Breakthrough bleeding
- Weight gain
- Acne
- Hirsutism
- Thromboembolism
- Pulmonary embolism
- Stroke
- Hypertension
- Genital carcinomas
- Gall bladder disease
- Breakthrough bleeding
- Weight gain
- Acne
- Hirsutism
Are all side effects of what drug?
Oral contraceptives
Describe the MOA of Leuprolide
It’s a GnRH analog that acts on the pituitary gland GnRH receptors it has both pulsatile & continuous forms