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
Describe pulsatile leuprolide
it’s a GnRH agonist to increase FSH & LH in pregnancy
Describe continuous leuprolide
A tumor flare (agonist) followed by a decrease in FSH & LH antagonists
Describe the MOA & Clinical uses of Ganirelix, cetrorelix, abarelix, & dagarelix?
MOA:
they are GnRH receptor agonists t=which when combined with GnRH analogs like leuprolide they can be used to avoid a tumor flare
Rx:
Advanced prostate cancer
Endometriosis
MOA:
they are GnRH receptor agonists t=which when combined with GnRH analogs like leuprolide they can be used to avoid a tumor flare
Rx:
Advanced prostate cancer
Endometriosis
Ganirelix, cetrorelix, abarelix, & dagarelix
What are the side effects of Leuprolide?
Hypogonadism
Nausea/vomiting
Erectile dysfunction
Decreased libido
Hypogonadism
Nausea/vomiting
Erectile dysfunction
Decreased libido
Are the side effects of what drug?
Leuprolide
Leuprolide lacks libido :(
What are the clinical uses of Leuprolide?
Infertility
Endometriosis
Prostate cancer
Precocious puberty
Uterine fibroids
Uterine fibroids
Infertility
Prostate cancer
Precocious puberty
Prostate cancer
Endometriosis
Are all side effects of what drug?
Leuprolide
Describe the MOA of Flutamide
A non-steroidal competitive inhibitor at the androgen receptors (decrease testosterone)
What are the side effects of Flutamide?
Gynecomastia
Breast tenderness
Liver damage
What are the clinical uses of Flutamide?
Prostate cancer
Acne
Female Hirsutism
PCOS (test symptoms)
Prostate cancer
Acne
Female Hirsutism
PCOS (test symptoms)
Are all side effects of what type of endocrine drug?
Flutamide
Describe the MOA of Finasteride
It inhibits 5-reductase at androgen receptors to decrease the conversion of testosterone to DTH
What are the side effects of Finasteride?
Gynecomastia
Sexual dysfunction
What are the clinical uses of Finasteride?
BPH
Male-pattern baldness
Men use Finastride to look fine
BPH
Male-pattern baldness
Can be treated with what endocrine drug?
Finasteride
Describe the MOA of Oxytocin
It stimulates the uterine smooth muscle to contract & it also had both vasopressor & antidiuretic effects
What are the clinical uses of Oxytocin?
Induce labor
Controlling uterine hemorrhage
Breast engorgement
Uterine inertia
Induce labor
Controlling uterine hemorrhage
Breast engorgement
Uterine inertia
Can all be treated with which endocrine-specific drug?
Oxytocin
What are the side effects of Oxytocin?
Hypotension
Arrythmias
Electrolyte imbalance
Increased uterine mobility
Decreased uterine blood flow
Abruptio placentae
Hypotension
Arrythmias
Electrolyte imbalance
Increased uterine mobility
Decreased uterine blood flow
Abruptio placentae
Are all side effects of which endocrine drug?
Oxytocin
Describe the MOA of ketoconazole
It inhibits steroid synthesis by inhibiting 17,20 desmolase & 17 hydroxylase)
&
It inhibits the CYPP450 enzymes needed for the synthesis of steroids at the Leydig cells (less testosterone)
What are the side effects of ketoconazole?
Gynecomastia
Amenorrhea
Gynecomastia & Amenorrhea are side effects of which endocrine-specific drug?
Ketoconazole
What are the clinical uses of ketoconazole?
PCOS
Adrenal carcinoma
Hirsutism
Breast & prostate cancer
Cushing’s
PCOS
Adrenal carcinoma
Hirsutism
Breast & prostate cancer
Cushing’s
Can all be treated with which endocrine-specific drug?
Ketoconazole
“CHAPP-B lips”
Describe the MOA of Levonorgestrel/progastrin’s
It’s administered before an LH surge to inhibit ovulation, it also affects the cervical mucus, tubal functioning, & endometrial lining
What is the clinical use of Levonorgestrel/progastrin’s?
Plan B
What are the clinical side effects of Levonorgestrel/progastrin’s?
Headaches
Nausea
Fatigue
Abdominal pain
Dizziness
Tender breasts
Headaches
Nausea
Fatigue
Abdominal pain
Dizziness
Tender breasts
Are all side effects of which endocrine-specific drug?
Levonorgestrel/progastrin’s
What are the zero order kinetics drugs
Phenytoin
Ethyl alcohol
Theophylline
Aspirin
Describe the MOA of Octreotide
It inhibits the release of GH, certain Gi & pancreatic hormones, & decreases splenic blood flow
What are the clinical uses of Octreotide?
Acromegaly
Carcinoid syndrome
Gastronome
Esophageal varices
Pituitary adenoma
Diabetic diarrhea
Acromegaly
Carcinoid syndrome
Gastronome
Esophageal varices
Pituitary adenoma
Diabetic diarrhea
Can all be treated with which endocrine-specific drug?
Octreotide
What are the side effects of Octreotide?
Loose stools
Steatorrhea
Malabsorption
Nausea
Flatulence
Gallstones
Loose stools
Steatorrhea
Malabsorption
Nausea
Flatulence
Gallstones
Are all side effects of which endocrine-specific drug?
Octreotide
ate(8) too much
Describe the MOA of Bromocriptine/cabergoline
It acts as a dopamine receptor agonist which are activated by lactotroph dopamine D2 receptors that cause lactin to be inhibited
What are the general side effects of Bromocriptine?
Dyskinesia
Psychosis
Nausea/vomiting
Dizziness
Nasal stuffiness
Orthostatic hypotension
Cold-induced vasospasms (Ergot effect)
What are the side effects of oral bromocriptine (Alendronate or Risectronate)
Gi upset
Gastric reflux
esophageal ulcers
Gi upset
Gastric reflux
esophageal ulcers
are side effects of which type of bromocriptine durgs
Oral:
Alendronate
Risechdronate
Dyskinesia
Psychosis
Nausea/vomiting
Dizziness
Nasal stuffiness
Orthostatic hypotension
Cold-induced vasospasms (Ergot effect)
Are side effects of which endocrine-specific drug?
Bromocriptine
Describe the following for calcitonin:
Clinical uses
Pagets disease & hypercalcemia
What are the clinical uses of Bromocriptine?
Hyperprolactinemia
Acromegaly
Galactorrhea
Parkinsons
BromoPIT-ine = pituitary conditions
Hyperprolactinemia
Acromegaly
Galactorrhea
Parkinsons
Can all be treated with which endocrine-specific drug?
Bromocriptine
What are the drug treatment options of acromegaly?
Bromocriptine/cabergoline
Octreotide
Somatostatin
Pevisomant
Bromocriptine/cabergoline
Octreotide
Somatostatin
Pevisomant
Can all be used to treat which condition?
Acromegaly
What are the triggers for G6PD deficiency?
1) Food (fava beans)
2) Antibiotics (Sulfa drugs, dapsone, nitrofurantoin, & isoniazid)
3) Anti-malarial (Primaquine, Chloroquine, & quinidine)
4) Aspirin & acetaminophen
1) Food (fava beans)
2) Antibiotics (Sulfa drugs, dapsone, nitrofurantoin, & isoniazid)
3) Anti-malarial (Primaquine, Chloroquine, & quinidine)
4) Aspirin & acetaminophen
Are all triggers for which condition?
G6PD deficiency
Nandrolone propionate
Nandrolone decanoate
Stanazolol
Oxandroline
Are all examples of which type of drug?
Anabolic steroids
Anabolic steroids (that you need to know x4)
Nandrolone propionate
Nandrolone decanoate
Stanazolol
Oxandroline
“PODS”
Describe the MOA for Clomiphene citrate
A non-steroidal used to induce ovulation. It’s a mixed agonist & antagonist for estrogen receptors & it acts on the hypothalamus to deplete ER & blocks the negative feedback of estradiol this results in higher levels of GnRH, FSH, & LH aka ovulation
A non-steroidal used to induce ovulation. It’s a mixed agonist & antagonist for estrogen receptors & it acts on the hypothalamus to deplete ER & blocks the negative feedback of estradiol this results in higher levels of GnRH, FSH, & LH aka ovulation
Describes the MOA for which drug?
Clomiphene citrate
What are the clinical uses & side effects of clomiphene citrate?
Uses:
Infertility
Side effects:
1) Multiple births
2) Hot flashes
3) Allergic dermatitis
4) Visual disturbances
Uses:
Infertility
Side effects:
1) Multiple births
2) Hot flashes
3) Allergic dermatitis
4) Visual disturbances
Describe the use of which drug ?
Clomiphene citrate
Describe the following for cushings:
What are the treatment options?
What is the diagnostic test?
What are the symptoms?
Apart from cancer or a fungus what can cause it (in babies)
Rx:
surgery to remove the adenoma
OR
Ketoconazole (antifungal) to block ergosterol synthesis of the fungi
Test:
Dexamethasone suppression test
Side effects:
1) Gynecomastia (ketoconazole_
2) Buffalo hum & moon face
3) purple striae
4) Hyperpigmentation (MSH)
Other cause:
Glucocorticoids which increase annexin-1 (lipocortin) phospholipase A2 inhibition
Corticosteroids have impacts on various systems:
What are the impacts of corticosteroids on the carbohydrate system?
Hyperglycemia (more gluconeogenesis & less peripheral uptake) be careful with diabetics
Corticosteroids have impacts on various systems:
What are the impacts of corticosteroids on the lipid metabolism system?
They cause redistribution of fa giving the classic buffalo hump & moon face appearance (careful with long tern use!)
Corticosteroids have impacts on various systems:
What are the impacts of corticosteroids on the calcium metabolism system?
It decreases intestinal absoprtion & increases renal excretion meaning there’s a high risk of developing osteoporosis
Corticosteroids have impacts on various systems:
What are the impacts of corticosteroids on the protein metabolism system?
causes a negative nitrogen imbalance which can lead to muscle aches & eventual myopathy in long term use
