Final Flashcards by G X

OXT

synthesized by magnocellular neurons, released through post. pituitary into general circulation
mech. stim (↑ pressure of cervix/myometrial contractions/suckling stim) triggers secretion from pituitary → stimulates OXT Rs in uterus/smooth m. of milk ducts in mammary glands = ↑ contraction
positive feedback: mechanoreceptors send impulses to hypot = ↑ OXT
also bonding effect

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vasopressin

synthesized by magnocellular neurons, released through post. pituitary into general circulation
↑ blood osmolarity/↓bp/↓blood vol triggers secretion from pituitary
kidneys: insertion of aq-2 channels = ↑ water reabsorption
vasculature: vasoconstriction
anterior pituitary: ACTH release

inhibited by alcohol

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pulsatile release from somatotrophs in anterior pituitary
bone: induces growth (postnatal)
muscle: ↑ aa uptake
adipocytes: ↑ lipolysis + ↓ body fat
liver: secretion of IGF-1

therapeutic use: replacement therapy - inj
tx of pituitary dwarfism + adult GH deficiency, short stature of Turner’s syndrome

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GH regulators

GHRH: positive central regulator = ↑ gene expr, ↑ GH release, induces somatotroph growth
STT: neg central regulator = ↓ GH release
ghrelin: pos peripheral reg = ↑ GH release from somatotrophs, ↑ GHRH + ↓ STT
IGF-1: neg peripheral reg = ↓ GHRH + ↑ STT, ↓ GH release
GH: autocrine factor - neg feedback

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pegvisomant

recombinant GH antagonist
tx of acromegaly

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octreotide

STT receptor agonist
tx of acromegaly + gigantism

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cortisol

circadian rhythm/stress induce hypot. release of CRH → corticotrophs = release of ACTH → synthesis of cholesterol in adrenal cortex = ↑ cortisol
negative feedback = inhibit CRH + ACTH → terminate stress response
bound to CBG (+ albumin) = inactive
inactivated by 11βHSD2 in kidney to cortisone; reactivated by 11βHSD1 in liver

release from CBG - cross cell membrane - binds GR → translocation to nucleus → dimerizes = genomic effects (transactivation or transrepression)

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17α hydroxylase

metabolism of pregnenolone in z. fasciculata + reticularis = involved in cortisol + androgen synthesis
inhibited by ketoconazole in tx of Cushings and prostate cancer

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21β hydroxylase

metabolism of pregnenolone in z. fasciculata + glomerulus = involved in cortisol + aldosterone synthesis
genetic mutation or immune response = primary adrenal insufficiency

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11β hydroxylase

metabolism of pregnenolone in z. fasciculata + glomerulus = involved in cortisol + aldosterone synthesis
inhibited by metyrapone = tx of cushings

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hydrocortisone

glucocorticoid replacement therapy
fails to replicate circadian rhythym of cortisol secretion
Chronocort = better mimic → tx for congenital adrenal hyperplasia

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prednisone

4x ↑ potency = greater affinity for GR receptor than cortisol

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dexamethasone

30x ↑ potency = greater affinity for GR receptor (no MR interaction

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vamolorone

selective glucocorticoid receptor modulator
favours transrepressing actions (anti-infl) of GR over transactivating (side effects)

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ketoconazole

antifungal, inhibitor of 17α hydroxylase
tx of Cushing’s disease - ↓ synthesis of cortisol + androgens
side effects: ↑ P and aldosterone

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metyrapone

inhibitor of 11β hydroxylase = ↓ cortisol + aldosterone
tx of Cushing’s disease
side effects: chronic use may cause hirsutism + hypertension

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mifepristone

GC antagonist (high affinity for GR)
tx of inoperable patients with ectopic ACTH secretion or adrenal carcinoma

SPRM: selective P antagonist → ↓ embryo implantation
emergency contraception - single dose in late follicular phase inhibits LH surge = no ovulation
combined with misoprostol = medical 1st trimester abortion

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estrogen

converted from androstenedione by aromatases
promote females sex development, growth, + endometrial proliferation
↑ binding proteins, ↑ HDL, ↓ LDL, kidney: salt + water retention
therapeutic uses: replacement therapy, contraception, menopause
adverse effects: ↑ cancer risk (breast, endometrial), thrombosis, edema

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anastrozole

antiestrogen = inhibitor of aromatase → ↓ E synthesis
tx of early + advanced ER+ reast cancer in postmenopausal women
no ↑ risk for uterine cancer or thrombosis

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clomiphene citrate

SERM → blocks ERs in hypot. + pit. - no negative feedback = ↑ gonadotropins
tx: induce ovulation, infertility, amenorrhea, PCOS
adverse effects: ovarian cysts, hot flashes, multiple births

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tamoxifen

SERM, prodrug (CYP2D6 → endoxifen)
combined with SSRIs (↓ CYP2D6) to ↓ hot flashes
tx of breast cancer; osteoporotic
adverse effects: ↑ risk of uterine cancer, blood clots

raloxifen

SERM = neutral in uterine tissue = no ↑ risk of cancer
still risk of blood clots

fulvestrant

SERD → binds ER monomer + prevents dimerization = degradation through ubiquitin pathway
tx of metastatic ER+ breast cancer
inhibits growth of tamoxifen-resistant tumors

PROTACs

proteolysis targeting chimeras = bind ER + E3 ligase = induce ubiquitination → degradation of ER
tx of ER+ breast cancer

progesterone

bound to albumin facilitates implantation + pregnancy maintenance; development of mammary gland; immune role; neuroprotective abnormal P responses: endometrial cancer, endometriosis, breast cancer, uterine fibroids, PMS/PMDD, lactation therapeutic uses: hormonal contraception, menopause, dysmenorrhea, endometriosis

ulipristal acetate

SPRM tx of uterine fibroids; emergency contraceptive - prevent/delay ovulation) caused liver damage

levonorgestrel

Plan B - progestin = emergency contraceptive prevents/delays ovulation + impairs luteal function

testosterone

secreted by Leydig cells when stimulated by LH bound to SHBG therapeutic uses: replacement therapy (hypogonadism: 1 = ↓T, ↑FSH/LH; 2 = ↓FSH/LH → ↓ T; pituitary deficiency, aging); protein anabolic agents; osteoporosis antiandrogens: tx of benign prostatic hyperplasia, prostate cancer

abiraterone acetate

2nd gen antiandrogen → inhibits 17α hydroxylase and 17, 20 lyase tx of androgen dependent prostate cancer adverse effects: cortisol deficiency

finasteride

5α reductase inhibitor = prevents T conversion to DHT tx of BPH; ↓ risk of impotence, infertility, ↓ libido

flutamide

competitive antagonist of AR tx of prostate cancer → mutation of AR can cause resistance

darolutamide

2nd gen AR blocker inhibits both WT and mut AR; more potent

SARMs

tx for osteoporosis (selective for bone) → attracted sports doping risks: ↑ heart attack/stroke, hallucinations, infertility

AAS

mimic T ↑ muscle mass + strength many adverse effects

cocaine

ester local anesthetic metabolism by plasma cholinesterase to PABA short half life

lidocaine

amide local anesthetic high protein binding metabolized in liver, slower = can accumulate max safe dose = 5mg/kg

bupivocaine

cardiotoxic → R(+) binds cardiac Na+ channels max safe dose = 2mg/kg

sevoflurane

inhalational anesthetic

propofol

IV anesthetic rapid onset (lipid soluble) + emergence (rapid clearance) anti emetic + anticonvulsant positive allosteric modulator of GABA A receptor → ↑ Cl- mvt = inhibition

ketamine

IV anesthetic NMDA R antagonist analgesia + (dissociative) anesthetic CV stability: ↑ hr + bp

montelukast

LTB4 antagonist

misoprostol

synthetic PGE1 uses: labor induction, tx of gastric ulcers

glucocorticoids

induce lipocortin = inhibit PLA2 (indirect inhibition of COX)

NSAIDs

analgesic, anti pyretic, anti inflammatory inhibit COX = ↓ PG synthesis inhibit PGE2 in hypothalamus = antipyretic action adverse effects: gastric ulcers

ASA

anti infl: ↓ adhesion + migration of immune cells; prevent infl cascade anti pyretic: ↓ PGE2 in hypot antiplatelet: irreversible antagonist of TXA2 in platelets (low dose = ↓ CV risk) risks: gastric irritation, Reye's Syndrome, renal effects

ibuprofen

more potent than ASA = analgesia at lower dose (↓ risk of gastric ulcers) ↑ risk of hypertension

indomethacin

inhibits both COX + PLA2 tx of gout

celecoxib

selective COX2 inhibitor no antiplatelet action, ↓ gastric irritation tx of arthritis risk: ↑ MI/stroke

acetaminophen

analgesic + anti pyretic (less effect on COX) tx of mild pain, fever in children (↓ risk of Reye's) liver toxicity → buildup of toxic metabolite

N-acetylcysteine

tx of acetaminophen-induced liver toxicity

hormonal contraceptives

progestin: ↓GnRH = ↓LH = no ovulation; ↓ sperm survival estrogen: ↓ GnRH = ↓ LH = no ovulation; prevent development of dominant follicle

prostate cancer

preventative/early stage → tx = HRT (↑T) advanced → tx = antiandrogens