Final Exam Structures

T4, used for hypothyroidism

Propylthiouracil, used for hyperthyroidism, inhibits TPO and deiodinase 1, safe in pregnancy

Methimazole, used for hyperthyroidism, inhibits TPO only, not safe in pregnancy, 1 st choice drug

gonadorelin (GnRH)

Nafarelin, GnRH Agonist, nasal formulation, 200x more potent than GnRH, much longer t1/2 than GnRH

Triptorelin, GnRH agonist, injectable, 100x more potent than GnRH, variable half-lives

leuprolide, GnRH agonist, 15x more potent than GnRH

Goserelin, GnRH agonist, longest t1/2 (4.9hrs), 10x more potent than GnRH

Histrelin, GnRH agonist, typically for delaying early onset puberty, 210x more potent than GnRH

GnRH antagonist peptide scaffold

amino acids 1-3 can be substituted by unnatural d-amino acids, amino acid 5 may be substituted, amino acid 6 substituted with D-amino acid, amino acid 8 may be substituted, amino acid 10 substituted with D-ala

Ganirelix, GnRH antagonist, fertility tx, daily subcut injection, t1/2 = 13-16 hrs

cetrorelix, GnRH antagonist, fertility tx, daily or single dose subcut injection, longer t1/2 than ganirelix (30-60 hrs)

degarelix, GnRH antagonist, preferred in tx of cancer, 2 step subcut injection, longest half life by far (41-70 days)

Elagolix, small molecule GnRH antagonist (oral), tx of endometriosis, shortest oral t1/2 (4-6 hrs)

relugolix, small molecule GnRH antagonist (oral), tx of prostate cancer, t1/2 of 24-45 hrs

Linzagolix, GnRH antagonist, tx of endometriosis, t1/2 15 hrs, 2 doses for partial vs full suppression

octreotide, SST analog, substitution at amino acid 8 (Trp → D-Trp)

lanreotide, SST analog, amino acid 7 (Phe → Tyr), amino acid 8 (Trp → D-Trp), amino acid 10 (Thr → Val)

pasireotide, SST analog, tx of cushing’s/acromegaly, subcut or IM injection, t1/2 7-12 hrs), excreted unchanged in urine

rimegepant, CGRP inhibitor, oral, tx of acute migraines and prevention, CYP3A4 metabolism

Vazegepant, CGRP inhibitor, nasal spray, tx of acute migraines

ubrogepant, CGRP inhibitor, oral, tx of acute migraines, CYP3A4 metabolism, shortest t1/2

Atogepant, CGRP, oral, prevention of migraines, CYP3A4 metabolism

serotonin

L-tryptophan (precursor to serotonin)

melatonin

Frovatriptan, serotonin analog (5HT1B/1D), tx of acute migraines, longest t1/2 (26-30 hrs)

sumatriptan, serotonin analog (5HT1B/1D), tx of acute migraines, MAO mediated metabolism

zolmitriptan, serotonin analog (5HT1B/1D), tx of acute migraines

rizatriptan, serotonin analog (5HT1B/1D), tx of acute migraines, MAO mediated metabolism

almotriptan, serotonin analog (5HT1B/1D), tx of acute migraines, decreased CYP metabolism

naratriptan, serotonin analog (5HT1B/1D), tx of acute migraines

eletriptan, serotonin analog (5HT1B/1D), tx of acute migraines

lasmitidan, selective 5HT1F receptor agonist (NAAMA), tx of acute migraines, helpful in pts with CV risk due to lower vasoconstriction

dolasetron, 1st gen 5HT3 receptor antagonist, prodrug, tx of N/V, oral or IV formulation, may cause QT prolongation

Granisetron, 1st gen 5HT3 receptor antagonist, tx of N/V, oral or IV or transdermal patch formulations, longer t1/2

ondansetron, 1st gen 5HT3 receptor antagonist, tx of N/V, oral or IV formulations, can require multiple doses

tropisetron, 1st gen 5HT3 receptor antagonist, tx of N/V, oral or IV formulations, long t1/2 (once daily dosing)

palonosetron, 2nd gen 5HT3 receptor antagonist, causes 5HT3 receptor internalization, tx of N/V, significantly longer half life than 1st gen, IV formulation, lasts up to 1 week

metoclopramide, dopamine receptor antagonist, tx of N/V

olanzapine, antagonist at D2/5HT2c/5HT3 receptors, tx of chemo-induced nausea/vomiting, typically using in combo with 5HT3 antagonists and NK-1 antagonists

aprepitant, NK1 antagonist, prevention of chemo induced N/V, oral

fosaprepitant, NK1 antagonist, prevention of chemo induced N/V, prodrug, injectable

rolapitant, NK1 antagonist, prevention of chemo induced N/V, oral and injectable, super long t1/2 (could be single dose), no CYP interactions

netupitant, NK1 antagonist, prevention of chemo induced N/V, oral

fosnetupitant, NK1 antagonist, prevention of chemo induced N/V, injectable

benzocaine, local anesthetic (amino ester)

procaine, local anesthetic (amino ester), low potency (high max dose)

chloroprocaine, local anesthetic (amino ester), low potency (high max dose)

tetracaine, local anesthetic (amino ester), high potency (low max dose)

proparacaine, local anesthetic (amino ester)

lidocaine, local anesthetic (amino amide)

prilocaine, local anesthetic (amino amide)

mepivacaine, local anesthetic (amino amide)

bupivacaine, local anesthetic (amino amide), high potency (low max dose)

ropivacaine, local anesthetic (amino amide)

inhaled general anesthetic

inhaled general anesthetic

inhaled general anesthetic

inhaled general anesthetic

inhaled general anesthetic

inhaled general anesthetic

propofol, iv general anesthetic, general purposes, metabolized in liver via glucuronidation

etomidate, iv general anesthetic, general purposes, metabolized in blood via esterase activity

ketamine, iv general anesthetic, used for short duration sedation, can cause hallucinations, CYP mediated metabolism

thiopental, iv general anesthetic, used for lethal injection

methohexital, iv general anesthetic, used fro electroconvulsant therapy (ECT)

midazolam, benzodiazepine (GABA), used for anterograde amnesia and anxiolytic for surgery

fentanyl, opioid, pain management for surgery

succinylcholine, NMJ blocker, temporary paralysis of skeletal muscles for surgery

dexmedetomidine, central alpha2 agonist, sedation for surgery

dantrolene, prevents calcium release from SR resulting in lower muscle contraction, treats malignant hyperthermia

cholestane

pregnane

androstane

cortisol

progesterone

testosterone

estradiol

glucocorticoid, topical

glucocorticoid, oral

glucocorticoid, prodrug

glucocorticoid, topical, low-medium potency

glucocorticoid, topical, high potency

glucocorticoid, ophthalmic, soft drug

glucocorticoid, inhaled/intranasal

glucocorticoid, inhaled/intranasal, prodrug

glucocorticoid, intra-articular injection

glucocorticoid, injectable

glucocorticoid, injectable

fetal estrogen, found in oral combo contraception

conjugated estrogen, used for menopause

tamoxifen, SERM, antagonist at breast tissue, tx of breast cancer, metabolized to more potent active metabolite via CYP2D6/3A4

ospemifene, SERM, active metabolite for breast cancer

raloxifene, SERM, antagonist at breast and agonist at bone, tx of osteoporosis with reduced breast cancer risk, BBW for DVT and stroke

bazedoxifene, SERM, used in combo with conjugated estrogen, tx of osteoporosis

clomiphene, anti-estrogen, tx of ovulation disorders

fulvestrant, SERD, IM injection, tx of breast cancer

elecestrant, SERD, oral, tx of breast cancer

exemestane, noncompetitive aromatase inhibitor