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Pharmacology - Final - Part 16

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davidwurbel7's version from 2016-08-14 07:13

Endocrine Pharmacology

Question Answer
Excessive GH before the fusion of the growth end plates causesGigantism
Excessive GH after the fusion of the growth end plates causesAcromegaly
Deficiency of GH causesPituitary Dwardism
The mechanism of action through releasing of (Insulin Like Growth Factors) or somatomedinsGH
Deficiency of IGFLaron Dwarfism
Large peptide molecule given s.c. Recombinate preparation of GHSomatropin
Uses include pituitary dwarfism, catabolic stares with excess protein loss (severe burns, chronic renal failure, osteoporosis, bed ridden patients, Prader-Wilii Syndrome, Turners, Intra Uterine Growth Hormone (IUGH)GH
Use Somatomedin or IGF-1 analogues MecaserminLaron Dwarfism
Laron dwarfism is treated with thisSomatomedin or Mecasermin
Preparation of this hormone (drug) has very short half life (1-3 minutes)Somatostatin
This drug also effects GI system in addition to the pituitarySomatostatin
A synthetic analogue of somatostatin that is 45 times more potent and has a longer half life (80 minutes)Octreotide
Side effects include gall stones and steatorrheaOctreotide
Uses include acromegaly, carcinoid tumors / carcinoid syndrome, esophageal varices, diabetic diarrheaOctreotide
This drug can be use as an alternative to octreotide for esophageal varicesDesmopressin
A GH antagonist that can be used to treat acromegalyPegvisomant
This drug does reduce the GH levels. It may actually increase the GH levels but no effect of GH is seen in the patientPegvisomant
Released from Anterior pituitary. Release is under the control of PRIH. Excess prolactin produces Hyperprolactenemia which is characterized by amenorrhea, infertility, Galactorrhea, Gynecomastia and loss of libidoProlactin
Prolactin release inhibitory hormone (PRIH)Dopamine
Bromocriptine and Cabergoline are examples of this class of drugsDopamine Agonists
Secreting adenoma, drugs such as antipsychotics and antiemetics and hypothyroidism are causes for thisHyperprolactinemia
Decreases prolactin release, Increases GH in normal persons but decreases GH in AcromegalyBromocriptine or Cabergoline
Uses for this drug include Hyperprolactenemia, Galactorrhea, Acromegaly, Parkinsonism. And to suppress milk production in stillborn casesBromocriptine or Cabergoline
In Male for testosterone synthesisLH
In Male for spermatogenesisFSH
In Female for Graffian follicle stimulation and release of estrogenFSH
In Female for ovulation and increases lutenization and release of progesteroneLH
GnRH agonist released in pulsatile mannerGonadorelin
Drug used for treatment of hypogonadism, delayed puberty, and cryptorchismGonadorelin
GnRH agonist released in continuous mannerLeuprolide
GnRH agonist that simulates the gonadsGonadorelin
GnRH agonist that suppresses the gonadsLeuprolide
Drug used for treatment of cancer of the prostate and breast, IVF, precocious puberty, fibroid uterus and endometriosisLeuprolide
DOC in endometriosisDanazole
Only suppression and no initial stimulation of gonadsGnRH Antagonists
Cetrorelix and Ganirelix are examples of this class of drugsGnRH Antagonists
Used to control ovarian hyperstimulation as a part of assisted reproductive procedure in IVFGnRH Antagonists
Hormone required for initiation /facilitation of the labor. Contracts upper part and relaxes the lower part of uterus thus facilitates fetal expulsionOxytocin
Used to induce labor to have early vaginal delivery in PET, postmaturity, Rh problems, uterine inertia and incomplete abortion. Can be used in post partum hemorrhage but better drugs are availableOxytocin
DOC for post partum hemorrhageErgonovine
Adverse effects include uterus rupture in excess dose or in obstructed laborOxytocin
Produces continuous contractions of uterus and contracts both upper and lower part which can lead to fetal asphyxiaErgonovine
Used for post partum hemorrhage and placental retentionErogonovine
Term for drugs used to induce laborEcbolic Agents
Term for drugs that are uterine relaxants are called asTocolytic Agents
Beta-2 agonists , alcohol and calcium channel blockers are examples of these class of drugsTocolytic Agents
These drugs are used to postpone the labor in premature deliveries Tocolytic Agents
V1 receptors are present hereBlood Vessels
V2 receptors are present hereRenal Collecting Duct
Vasopressin acts more on this receptorV1
Desmopressin acts more on this receptorV2
Twelve times more potent, ,longer acting ,used as intranasal spray. more commonly usedDesmopressin
Used for Diabetes insipidus (neurogenic), nocturia, bleeding oesophageal varices, haemophilia and vonWillbrand’s diseaseDesmopressin
Used to treat lithium-induced nephrogenic diabetes insipidusAmiliride
Used to treat nephrogenic diabetes insipisdus of unknown causeThiazides
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Gonadotropins

Question Answer
Used to treat infertility due to anovulation, polycystic ovarian disease - menotropins + hCG - induce ovulation, hypogonadism and cryptorchismGonadotropins
Used in conditions where you want to stimulate gonads. Released in body in pulsatile mannerGonadorelin
GnRH agonist released in continuous manner. Initially increases production of FSH and LH and then reduces FSH and LH due to receptor down regulationLeuprolide
GnRH antagonists that block the GnRH receptors. Only suppression and no initial stimulation of gonadsCetrorelix and Ganirelix
Physiological effect of this hormone is proliferation of endometrial liningEstrogen
Ethinyl estradiol, Mestronol and Quinestrol are examples of these drugsSynthetic steroidal Estrogens
A synthetic non steroidal estrogenDiethyl Stilbesterol
DOC in endometriosisDanazole
Used as hormonal contraceptives and used as Hormonal replacement therapy (HRT) in menopauseEstrogen
This is characterised by irritability, loss of skin turgor, dry skin, dry vagina, mood instability and fragile bones, osteoporosis, frequent bone fracture, vasomotor disturbances, urogenital atrophy ,osteoporosis, skin changes, depression, increase risk of MI and strokePost Menopausal Syndrome
Adverse effects include nausea, vomiting, migraine, increased risk of myocardial infarction, stroke, gall stones, pulmonary embolism, carcinoma of breast and endometrial carcinomaEstrogen
SERMsSelective Estrogen Receptor Modulators
Clomiphine citrate, Tamoxifen, Raloxifen are examples of this class of drugsAnti-Estrogen and SERMs
This drug acts as competitive antagonist at estrogen receptors in pituitary and hypothalamus. Interferes with negative feedback of estrogen on hypothalamus and pituitary. This increases the secretion of GnRH leading to increased FSH and LH and thus the chances of ovulationClomiphine Citrate
This drug is used when an increase of FSH and LH hormones are neededClomiphine Citrate
This drug blocks the estrogen receptor on breast. Therefore best used in Breast cancer. Because of agonistic effect on endometrium, this drug has a risk of endometrial cancerTamoxifen
The use of this drug has a risk of endometrial cancerTamoxifen
The use of tamoxifen to treat breast cancer has a risk of thisEndometrial Cancer
This drug is used to treat osteoporosis in post menopausal women. There is no risk of carcinoma of endometrium or breast because this drug has agonistic action only on the bone and antagonistic actions on breast and uterusRaloxifen
This drug is an aromatase inhibitor. Aromatase inhibitors work by inhibiting the action of the enzyme aromatase which converts androgens into estrogens by a process called aromatizationAnastrozole
This drug can be used in estrogen-sensitive breast cancers, following surgery or metastasis more so in postmenopausal womenAnastrozole
This drug is mostly used against invasive and/or metastatic breast cancersAnastrozole
Medroxy progesterone acetate, Megestrol and Hydroxy progesterone caproate are examples of this class of drugsProgesterone Derivatives
Norethindrone, Levonorgestrel, Desogestrel, and Norgestimate are examples of this class of drugs19-Nortestosterone Derivatives
Uses include hormonal contraceptives and HRT (counteract the adverse effect of estrogens i.e endometrial cancer)Progesterone Preps
Adverse effects include breast engorgement, irregular bleeding, lowers HDL levels – atherogenesis seen mostly with more androgenic progestins such as MedroxyprogesteroneProgesterone Preps
The mechanism of action is competitive inhibition of progesterone receptors glucocorticoid receptor antagonistMifepristone (RU486)
Uses of this drug include medical termination of early pregnancy - given along with misoprostol - dislodges fetus and lowers hCG, causing cervical softening. Used as postcoital emergency contraceptive pillMifepristone (RU486)
This drug contains Ethinyl estrodiol or Mestronol plus one of the progestinsCombined Hormonal Contraceptive Pills
Serious adverse effects include deep vein thrombosis, raise in BP, gall stones and increased chances of MI, especially with smokingContraceptive Pills
Nandrolone decoanate, Oxandrolone and Oxymetholone are examples of this class of drugsAnabolic Steroids
These drugs can be used for osteoporosis anaemia associated with malignancy, renal failure, and aplastic anaemia. Catabolic states. Abused in sportsAnabolic Steroids
A 5-alpha reductase inhibitor. Used in BPH and hirsutism. 5-alpha reductase is required for activation of testosterone to dihidrotestosteroneFinasteride
An antiandrogen drug that is a receptor blocker used in prostatic cancerFlutamide
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Corticosteroids

Question Answer
CortisolGlucocorticoids
AldosteroneMineralocorticoids
Estrogen, Progesterone, TestosteroneSex Steroids
The mechanism of action is the modification of gene transcriptionSteroids
Increases renal Na+ reabsorption and water retention leading to edema and increases K+ and H+ excretion in urine leading to hypokalemia and metabolic alkalosisMineralocorticoid
Short and rapid acting (t ½ less than 12 hours) with equal glucocorticoid and mineralocorticoid activityHydrocortisone (Cortisol)
Intermediate acting: t ½ 12-36 hours. More potent, more glucocorticoid activityPrednisolone
Intermediate acting: t ½ 12-36 hours. No mineralocorticoid activity. Inhalation preparationTriamcinolone
Intermediate acting: t ½ 12-36 hours. Inhalation preparationFluprednisolone
Mineralocorticoid with no glucocorticoid activityFludrocortisone
Long acting: t ½ around 36 hours. Most potent, no mineralocorticoid activityBetamethasone and Dexamethasone
Short acting. G:M ratio is 1:1 having equal glucocorticoid and mineralocorticoid activityCortisone, Cortisol and Hydrocortisone
Intermediate action. Mainly glucocorticoid activityPrednisone and Prednisolone
Long acting. Only glucocorticoid activityBetamethasone and Dexamethasone
Only have mineralocorticoid activityFludrocortisone
Beclomethasone, Budesonide, Fluticasone and TriamcinoloneInhalation Steroids
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Question Answer
Chronic adrenal insufficiency (Addison's disease)Hydrocortisone + Fludrocortisone
Acute adrenal insufficiency (Addisonian crisis)Hydrocortisone
Diagnosis of Cushing’s syndromeDexamethasone
In premature labor to help prevent respiratory distress in new bornBetamethasone
DOC for all acute and emergency situationsHydrocortisone
Glucocorticoid antagonist that is safer to use in pregnancyMetyrapone
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Question Answer
Adverse effects include peptic ulcers, Osteoporosis, Precipitation of diabetes, edema, Muscle wasting, fragile skin, purple striae, Precipitates infection-Tuberculosis, candidiasis, Cataract, Cushing’s habitus, Delayed wound healing and HPA axis suppressionCorticosteroids
Malaise, fever, weakness, joint pain, reactivation of disease, Addisonian crisisHPA Axis Suppression
Inhibits 11-hydroxylation and thus the synthesis of cortisol. Used in Cushing's syndrome, especially in pregnant women, since this is the only safe antagonist.Metyrapone
Mineralocorticoid antagonist Used in treatment of primary hyperaldosteronism (Conn’s syndrome) and HirsutismSpironolactone
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