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Pharmacology II Exam 4
Pharmacology II Exam 4
101
Pharmacology
Professional
04/09/2012

Additional Pharmacology Flashcards

 


 

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Term
Hypothalamus Function
Definition
Controls food/water intake, body temp., diurnal rhythms, CV function
Term
Oxytocin (receptor)
Definition
Gq coupled receptor
Term
Oxytocin
Definition
increases production of prostaglandins that stimulate contraction of uterine smooth muscle and mammary myoepithelial cells resulting in induction of labor and milk ejection but also used for stopping post pardem hemorrhage.
Term
Vasopressin (receptor)
Definition
V1 and V2 receptors; V1 found on vascular smooth muscle and cause vasoconstriction; V2 found on renal tubule cells and cause increased water permeability of the collecting tubules
Term
Vasopressin
Definition
causes increased synthesis of aquaporin-2 proteins for long-term effect; causes insertion of aquaporin-2 into the apical membrane of the collecting duct cells for short-term effect; also causes vasoconstriction to a much lesser extent and can be used to treat hypovolemic shock
Term
Desmopressin
Definition
Synthetic analog that is more selective for the V2 receptor and longer acting due to increased half-life
Term
ADRs of vasopressin
Definition
peripheral vasoconstriction, arrhythmias, GI cramps, headache, water intoxication
Term
Corticotropin Releasing Hormone (CRH)
Definition
Adrenocorticotropic Hormone (ACTH)
Term
Thyrotropin Releasing Hormone (TRH)
Definition
Thyroid-Stimulating Hormone (TSH)
Term
Gonadotropin Releasing Hormone (GnRH)
Definition
Follicle Stimulating Hormone (FSH/Follitropin) and Leutinizing Hormone (LH/Lutropin)
Term
Hrowth Hormone Releasing Hormone (GHRH)
Definition
Somatotropin (Growth Hormone)
Term
Growth Hormone (stimulators)
Definition
Secretion also stimulated by Dopamine, 5-HT (Serotonin), hypoglycemia, stress, exercise, sleep, ingestion of protein rich food, GHRH
Term
Growth Hormone (Physiologic Effects)
Definition
Increased production of IGF-1 which increases protein synthesis, muscle mass, Ca retention and long bone growth, lipolysis of fat, gluconeogenesis; neg feedback by increased IGF-1, FFA, and GH levles
Term
GH/IGH-1 (receptor)
Definition
Tyrosing kinase receptors of the JAK/STAT superfamily
Term
Prolactin
Definition
Stimulates milk production when levels of estrogen, progesterone, corticosteroids, and insulin are correct
Term
Somatropin/Somatrem
Definition
recombinant human growth hormones (rhGH)
Term
Acromegaly
Definition
Caused by pituitary adenomas which cause hypersecretion of GH
Term
Bromocriptine
Definition
Dopamine receptor agonist used to treat acromegaly which causes paradoxical decrease in GH production; may work via a negative feedback mechanism; Also used to treat hyperprlactinemia b/c dopamine stops prolactin secretion
Term
Somatostatin (receptor)
Definition
SSTR1-5 Receptor
Term
Somatostatin
Definition
inhibits the release of GH, glucagon, insulin, and gastrin
Term
Octreotide (Sandostatin)
Definition
Acromegaly treatment; GH antagonist; blocks release of GH from ant. pit.; more selective for GH inhibition than insulin inhibition
Term
Lanreotide (Somatuline)
Definition
Acromegaly treatment; GH antagonist; blocks release of GH from ant. pit.; more selective for the SSTR 2&5 which mediate GH inhibition
Term
Pegvisomant
Definition
Acromegaly treatment; GH analog that blocks the GH receptor instead of GH release; prevents receptor dimers from forming and leads to reduced IGF-1 level
Term
Drugs that induce hyperprolactinemia
Definition
Antipsychotics, Antidepressants, Opiates, Verapamil
Term
HPA axis function
Definition
Controls digestion, immune system, mood, energy use
Term
Corticotropin Releasing Hormone (receptor)
Definition
CRH recetpors(membrane-bound peptide receptor) on the anterior pituitary
Term
Pro-opiomelancortin (POMC)
Definition
precursor protein of adrenocorticotropic hormone
Term
Melanocyte-stimulatin hormone (MSH)
Definition
first 13-amino acid peptides of ACTH; cleaved from ACTH in the intermediate lobe of the hypothalamus; stimulates pigment production from melanocytes
Term
Adrenocorticotropic Hormone (receptor)
Definition
G-protein coupled receptor
Term
ACTH
Definition
maintains the functional integrity of the adrenal cortex and causes synthesis and release of mineralcorticoids, glucocorticoids, and androgens
Term
Testosterone (receptor)
Definition
Androgen receptor; nuclear receptor because testosterone is a steroid
Term
Glucocorticoid Function
Definition
Increase glucose levels; stimulate protein breakdown so AAs can be used for glucneo; Breakdown triglycerides so FFAs can be used by muscle and glycerol in glucneo; Stimulate liver to begin glucneo; prevent muscles and fat from taking in glucose; cause breakdown of muscle, bone, ct, skin; inhibit pro-inflammatory cytokine release from immune cells; induce insomnia, euphoria, depression
Term
Glucocorticoids (receptor)
Definition
made from cholesterol (steroid) so nuclear receptor
Term
Cushing's Syndrome
Definition
Primary hypercortisolism; Low ACTH High Cortisol
Term
Cushing's Disease
Definition
Secondary hypercortisolism; High ACTH High Cortisol
Term
Addison's Disease
Definition
Primary hypocortisolism; High ACTH Low Cortisol
Term
Sheehan's (pregnancy) or Simmond's disease
Definition
Secondary hypocrtisolism; Low ACTh Low Cortisol
Term
Mineralcorticoids (receptor)
Definition
Nuclear; steroid
Term
Fludrocortisone
Definition
synthetic mineralcorticoid used for the treatment of Addison's disease; binds to both the MR and GC receptor; most ADRs mediated through the MR receptor so not as bad as GCs
Term
Spironolactone
Definition
Aldosterone antagonist; binds MR and androgen receptor;
Term
GnRH (receptor)
Definition
G-Protein coupled recptor; peptide hormone
Term
Leuprolide
Definition
GnRH agonist; act indirectly by binding to autoreceptors on hypothalamus and causing negative feedback; act directly by binding to receptors on anterior pituitary and causing steady release of LH and FSH initially but there is a desensitiaztion effect and an interruption of the pulsatile release of these hormones
Term
Histrelin, Nafarelin, Triptorelin, Goserelin
Definition
GnRH agonists approved for differing indications
Term
Cetrorelix, Degarelix
Definition
GnRH antagonists; they block the GnRH receptors on the ant. pit. and prevent the release of LH and FSH.
Term
LH, FSH, and hCG (receptors)
Definition
G-protein coupled receptors; peptide hormones; hCG binds both LH and hCG receptors
Term
Phases of menstrual cycle
Definition
Follicular, ovulatory, luteal
Term
Estrogen binding proteins
Definition
α2-globulin, sex-hormone binding globulin, albumin
Term
Ethinyl estradiol, Estradiol valerate
Definition
Synthetic estrogens used for oral contraception or hormone replacement therapy
Term
Estrogen (receptor)
Definition
Nuclear receptors; ERα and ERβ
Term
Estrogen Function
Definition
Maintain blood vessel function, increase bone density, produce clotting factors, behavioral and mood effects, regulation of the menstrual cycle, function of female reproductive organs, development of female secondary sex characteristics
Term
Progesterone (receptor)
Definition
A and B receptors; nuclear receptors; lipid soluble so it has CNS effects
Term
Progesterone
Definition
Decreases estrogen-driven endometrial proliferation; increases body temp; causes drowsiness; decreases Na reabsorption by binding to MR and competing with aldosterone
Term
Ethinyl estradiol
Definition
combo contraceptive
Term
L-Norgestrel
Definition
combo contraceptive
Term
Desogestrel
Definition
combo contraceptive
Term
Combo contraceptives
Definition
Negatively feedback onto the hypothalamus and prevent the release of LH and FSH preventing ovulation; decrease ovary function and size
Term
L-Norgestrel; Medroxyprogesterone
Definition
the only progestin only contraceptive; causes thickening of the cervical mucus and endometrial changes
Term
Estrone, Equilin, Equilenin
Definition
the major forms of estrogen in premarin two of which are cytotoxins that cause DNA damage; used for hormone replacement therapy to alleviate the symptoms of menopause
Term
Clomiphene
Definition
Estrogen receptor partial agonist used as a fertility treatment; inhibits hypothalamic negative feedback and allowed continued production of FSH and LH and continued ovulation
Term
Follitropin alpha, Follitropin beta, Urofollitropin
Definition
FSH agonists used for fertility treatment
Term
5α-reductase
Definition
enzyme that converts testosterone to dihydrotestosterone (active metabolite)
Term
Aromatase
Definition
enzyme that converts testosterone to estradiol
Term
Oxandrolone, Nandrolone, Methyltestosterone
Definition
synthetic testosterone; 17α-alkylated androgens that bind to the androgen receptor and cause transcription
Term
Exemestane
Definition
Aromatase inhibitor; prevents the conversion of testosterone to estradiol
Term
Flutamide
Definition
Androgen receptor antagonist used to treat androgen sensitive tumors
Term
Raloxifene
Definition
estrogen receptor partial agonist used to treat osteoporosis and breast cancer
Term
Tamoxifen
Definition
estrogen receptor partial agonist used to treat breast cancer but not indicated for osteoporosis treatment
Term
1a-hydroxalase activity
Definition
enzyme that activates vitamin D in the kidney (converts Vitamin D to 1,25-dihydroxy-D)
Term
Hypercalcemia of Malignancy
Definition
causes hypercalcemia by (1) production of activated vitamin D by tumors (2) direct osteolysis of bone (3) PTH synthesis and release by tumor
Term
Jansen’s metaphyseal chondrodysplasia
Definition
Disorder where PTH receptor is activated in the absence of PTH
Term
Pseudohypoparathyroidism
Definition
Parathyroid produces sufficient PTH but there is a defect in the Gas subunit of the PTH receptor; no problem with PTH production
Term
Bisphosphonates
Definition
Bind to osteoclasts and prevent bone resorption; inhibit activation of Vit D3; Inhibit Ca transport in intestine; used to treat OP and hypercalcemia
Term
Cinacalcet
Definition
Calcimimetic; sensitizes the calcium receptors on the parathyroid and makes them more susceptible to neg feedback due to circulating calcium; treats hypercalcemia and hyperparathyroidism
Term
Thiazides
Definition
inhibit Na reabsorption and increase Ca reabsorption; treats hypocalcemia
Term
Calcitriol, Doxercalciferol, Paricalcitrol
Definition
Vitamin D metabolites used to increase serum calcium levels
Term
Thyroid function
Definition
important in growth and development, energy metabolism, body temperature
Term
Calcitonin
Definition
regulates calcium metabolism
Term
T3
Definition
binds cell surface receptors and cause increased uptake of glucose and amino acids; bind cytoplasmic binding protein leading to increased protein synthesis
Term
Perchlorate, Thiocyanate, Pertechnetate
Definition
monovalent anions that inhibit the thyroid's uptake of iodine
Term
Thyroid peroxidase
Definition
oxidizes iodide to iodine in the thyroid follicular cell
Term
Thionamides
Definition
Drugs that inhibit thyroid peroxidase and prevent oxidation of iodide to iodine and coupling of MIT and DIT
Term
Thyroxine binding globulin, Transthyretin
Definition
serum proteins that bind T3 and T4 to prevent their degredation
Term
Grave's Disease
Definition
stimulation of the thyroid in the absence of TSH by antibodies that mimic TSH produced by lymphocytes
Term
Methimazole, Propylthiouracil
Definition
Thionamides
Term
Goitrogens
Definition
Agents that decrease TH production
Term
Gull's Disease
Definition
Hypothyroidism
Term
Hashimoto's Thyroiditis
Definition
autoimmune destruction of the thyroid causing hypothyroidism
Term
Levothyroxine
Definition
T4 used to treat hypothyroidism
Term
Liothyronine
Definition
T3 used to treat hypothyroidism
Term
Insulin Glargine
Definition
Insulin that has a glycine attached to the end of the alpha chain and two arginines attached to the beta chain resulting in a soluble form at pH 4 that crystalized at the body's pH of 7.4. They begin as hexamers and finally break down to monomers for increased duration of action.
Term
Insulin Detemir
Definition
Insulin with long chain fatty acid attached that helps bind to albumin and increases duration of action
Term
Lispro, Aspart, Glulisine
Definition
fast acting insulins <15 min
Term
Regular insulin
Definition
insulin with onset of 30 min - 1 hr
Term
Glimepiride, Glipizide, Glyburide, Gliclazide
Definition
sulfonylureas; stimulate insulin release from the beta cells by binding to the sur1 protein and indirectly inhibiting the K channel stimulating insulin release
Term
Repaglinide, Nateglinide
Definition
meglitinides; stiumlate insulin release from the beta cells by directly binding the k channel blocking it and causing insulin release
Term
Metformin
Definition
biguanide; decrease hepatic glucose production (gluconeogenesis)
Term
Rosiglitazone, Pioglitazone
Definition
Thizolidinediones; improve peripheral insulin sensitivity by targeting the peroxisome proliferator receptors on the peroxisomes of adipose tissue and preventing carb metabolism. This reduces free fatty acid levels in the blood. Lower levels of fatty acids improve the performance of insulin in the periphery. These also increase the synthesis of adiponectin (Acrp30) which is supposed to increase sensitivity to insulin. Acrp30 is derived from adipose tissue.
Term
Acarbose, Meglitol
Definition
Alpha-glucosidase inhibitors; delay carbohydrate absorption in the gut by preventing/decreasing enzymatic hydrolysis of starch/carbohydrates
Term
Sitagliptin, Saxagliptin, Linapgliptin
Definition
DPP-4 inhibitors; following a meal, GLP-1 (incretin) is produced which causes insulin release and prevents the glucagon production in the pancreas. DPP-4 breaks down GLP-1 and these drugs inhibit DPP-4
Term
Exenatide (Byetta)
Definition
incretin agonist; mimics GLP-1 and GIP which causes release of insulin and prevents glucagon production in pancreas
Term
Liraglutide
Definition
incretin analog; mimics GLP-1 and GIP which causes release of insulin and prevents glucagon production in pancreas
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