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Glossary of Block 3 Pharm

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pyridostigmine
Carbamate, used in MG, binds to and block AChE for a 8-10 hrs.
neostigmine
Carbamate, used in MG, binds to and block AChE for a 8-10 hrs.
Parathion
Phosphate ion forms an extremely stable complex with AChE, ion released over period of days to weeks
echothiphate
Phosphate ion forms an extremely stable complex with AChE, ion released over period of days to weeks
Edrophonium
Short lived. Electrostatic attraction and hydrogen bonding at the active site of AChE
Succinylcholine
Depolarizes muscle endplate like ACh but for longer. Initial fasicullations, then muscle relaxing due to refraction.
Hemicholinium
Blocks reuptake of Choline, lowers ACh release.
Caribidopa
Carbidopa is an AAD inhibitor that cannot cross the blood-brain barrier so it acts to stop levodopa from becoming dopamine in the periphery, decreasing the unwanted side effects
Levodopa
converted to dopamine by AAD (aromatic L-amino acid decarboxylase
Bromocriptine
dopamine agonist, inhibits prolactin release!
pergolide
Dopamine Agonists
Tolcapone
Inhibits catechole-O-methyl transferase which degrades biogenic amines such as dopamine
entacapone
Inhibits catechole-O-methyl transferase which degrades biogenic amines such as dopamine
Selegiline
Irreversibly inhibit monoamine oxidase-B which is responsible for the breakdown of dopamine
Rasagiline
Irreversibly inhibit monoamine oxidase-B which is responsible for the breakdown of dopamine
benztropine
Block muscarinic receptors in the striatum, so ACh cannot bind.
This balances the cholinergic/dopaminergic activity in the basal ganglia
trihexyphenidyl
Block muscarinic receptors in the striatum, so ACh cannot bind.
This balances the cholinergic/dopaminergic activity in the basal ganglia
Amantidine
Antiviral agent that improves symptoms of Parkinson’s through unknown mechanisms
beclomethasone
Glucocorticosteroids
↓ production of leukotrienes and prostaglandins by inhibition of phospholipase A2 and negative expression of COX-2 genes
Used to treat mechanical back pain because of anti-inflammatory effects
hydrocortisone
Glucocorticosteroids
↓ production of leukotrienes and prostaglandins by inhibition of phospholipase A2 and negative expression of COX-2 genes
Used to treat mechanical back pain because of anti-inflammatory effects
prednisone
Glucocorticosteroids
↓ production of leukotrienes and prostaglandins by inhibition of phospholipase A2 and negative expression of COX-2 genes
Used to treat mechanical back pain because of anti-inflammatory effects
cyclobenzaprine
Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening
diazepam
Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening
methocarbamol
Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening
hydrocodone
Opioid Analgesics
μ-opioid receptor agonist
morphine, hydrocodone, fentanyl, meperidine
Opioid Analgesics
μ-opioid receptor agonist
amitriptyline
anti-neuritic pain relievers
Promote serotonergic and noradrenergic neurotransmission by inhibiting the reuptake of the neurotransmitter—helps to produce antinociceptive states
imipramine
anti-neuritic pain relievers
Promote serotonergic and noradrenergic neurotransmission by inhibiting the reuptake of the neurotransmitter—helps to produce antinociceptive states
Premarin
• An estrogen with a charged group that prolongs its half life
• Clinical uses—postmenopausal hormone replacement therapy
Heparin
• Promotes activity of antithrombin III which inactivates activated Factor X and thrombin
Warfarin
• Inhibits epoxide reductase and thus prevents vitamin K from being activated
• Vitamin K is a cofactor for many coagulation factors, w/o it the clotting cascade is essential inhibited
Trazodone
• Second generation heterocyclic that selectively inhibits serotonin uptake
• Clinical uses—depression
Baclofen
• Binds and activates GABAB receptors in CNS, decreasing tonic neural stimulation to muscles
• Clinical uses—muscle relaxant for MS or spinal cord lesions
Botulinum Toxin
• Prevents presynaptic ACh release by cleaving SNAP-25, leading to muscle paralysis
• Clinical uses—eyelid spasms, strabismus, facial wrinkles
methylprednisolone
glucocorticoid, treatment of acute demyelinating episodes in MS.
IFN-Beta
MS:
Downregulates MHC expression.
Inhibits proinflammatory cytokines
Increases regulatory cytokines
Inhibits T-cell proliferation
Glatiramer acetate (copaxone)
MS: reduces attack rate, severity

Binds MHC molecules, alters balance between pro and regulatory cytokines
Natalizumab
MS:
inhibits attachment of tCells to endothelial cells, preventing BBB crossing.
Mitoxantrone hydrochloride
MS:
Antineoplastic, interferes with RNA synthesis, inhibits DNA repair.
Azathioprine
MS:
Immunosupressant interferes with nucleic acid synthesis during S phase. Decreases relapse rate.
Methotrexate
MS: for relapsing MS.
DHFR inhibitor, anti inflammatory
betamethasone
Corticosteroid: induces development and maturation of fetus's lungs
Magnesium sulfate
seizure control in preeclampsia. Mg depressess CNS decreaseing amount of ACh released by motor neurons.
Misoprostol
uterine stimulant. Induces labor:

Synthetic Prostaglandin E, induces contractions. Also causes NO release opening cervix.
Labetolol
Anti hypertensive, beta and alpha1 adrenergic blocker. Give postpartum
Alpha methyldopa
HT in pregnancy. Anti adrenergic, converted to methylnorepinephrine substituting for NE. Inhibits vasoconstriction from brainstem.
hydralazine
HT emergencies. Vasodilator, lowers pressure by relaxing vascular smooth muscle... Alters calcium metabolism so muscle cannot contract.
Clomiphene
Inhibits negative feedback of estrogen on the hypothalamus and pituitary, thereby increasing the secretion of GnRH and FSH and LH to cause ovulation. It has been used successfully alone to treat infertility for more than 40 years and also used to increase the number of follicles to harvest in IVF
hCG and hMG
cause ovarian follicular growth and maturation.
promote maturation of the testes and spermatogenesis
Cabergoline
dopamine agonist with a long t½ of 65 hours approved by the FDA for the treatment of hyperprolactinemia and infertility
Estradiol/estrone/estriol
Naturally occurring estrogens, large first pass.
ethinyl estradiol
Synthetic estrogens, less first pass, effective orally
tamoxifen
selective estrogen receptor modulators (SERMS)

breast cancer
raloxifene
selective estrogen receptor modulators (SERMS)

breast cancer
mestranol
Estrogen: suppresses ovulation
etridronate/risedronate/alendronate/pamidronate
Bisphosphonates
Osteoporosis

1. inhibition of osteoclastic proton pump
2. decreased osteoclastic activity
3. increased osteoclastic apoptosis=cell death
Estrogens
causing imbalance between coagulation and anticoagulation, estrogens may produce thromboembolism, thrombophlebitis, myocardial infarction and cerebral and coronary thrombosis.
Toremifene
acts like tamoxifen but it does not cause endometrial cancers. The use of toremifene is restricted to post menopausal women with metastatic breast cancer
norethindrone
progestins :prevent implantation and make the cervix impenetrable to sperm
high dose estrogen
Post coital or emergency contraception
norplant
Progestin implant
Estring
deposits estrogen in vagina to treat vaginal atrophy and dryness, urinary incontinence
medroxyprogesterone, hydroxyprogesterone acetate, norethindrone, norgestrel
progestins:
1) Contraceptives – either in combination with estrogen, alone or sequentially.
2) dysfunctional uterine bleeding
3) treatment of dysmenorrhea – reduces the thickening of the uterine lining which makes prostaglandins that cause dysmenorrhea.
4) suppression of postpartum lactation for women who do not want to nurse
5) management of endometriosis
6) endometrial carcinomas.
mifepristone
(RU-486) is a progestin antagonist with partial agonist activity. Inhibits hCG to terminate pregnancy 85% successful
Progestin minipills
Main action of minipills is to make the uterus inhospitable for implantation
Finasteride/Flutamide/bicalutamide
Antiandrogens. Prostate treatment.
Desmopressin
ADH analog with no pressor effects . used to treat diabetes insipidus
octreotide
Analog GHIH to inhibit GH release. Giantism.

Also used to treat insulinoma.
Ghrelin
secreted by the stomach in a daily rhythm that closely mirrors normal food intake with 3 spikes at common meal times and at bedtime. stimulate appetite or the release of growth hormone
dexamethasone
synthetic glucocorticosteroid. Test for Cushings: feedback inhibits cortisol release in secondary Cushing’s by feedback inhibiting ACTH whereas dexamethasone does not reduce cortisol levels in primary adrenal tumors (or other aberrant sites) since these are not regulated by ACTH
Glucocorticoid withdrawal
Abrupt withdrawal causes Addison’s disease (adrenal insufficiency) that can be lethal. Withdrawal may cause exacerbation of the inflammatory disease because steroids are not curing the cause of the inflammation but only masking the symptoms. Steroids cause changes in the gene expression of enzymes making neurotransmitters in the brain. Withdrawal causes psychological changes as well as renewed inflammation. The dose must be tapered slowly and the patient must be watched closely.
levothyroxine
Synthroid
Primary and secondary hypothyroidism is treated by giving T4
glucagon injection
Emergency treatment: diabetic becomes unconsciousness - hypoglycemia treatment.
tolbutamide
Sulfonylureas:
1)stimulation of insulin release (inhibits KATP channel, depolarization causes insulin release).

Sulfonylureas can cross placenta DO NOT USE IN PREG.
2) reduction of serum glucagon
3) increased insulin binding to target cells.
6 ways to control blood glucose
1. lower glucose with insulin (subQ injections)
2. lower glucose with sulfonylureas = KATP channel blocker to release more insulin. Glyburide, glipizide, tolbutamide, glimepiride
3. lower glucose with repaglinitide, netaglinide, KATP channel blocker but not chemically a sulfonylurea, acts with digestive hormones postprandially.
4. insulin sensitizer - metformin – prevent plasma glucose from rising by blocking new glucose production (gluconeogenesis) in the liver and decreasing glucose absorption.
5. Insulin sensitizer - Troglitazone, Rosioglitazone –stimulates PPAR to reactivate insulin signaling.
6. Acarbose, Miglitol – prevents glucose uptake from the intestine brush border membrane.
7. Exenitide – GLIP-1 and GIP analog (subQ) increases insulin release, increases β cells proliferation, decreases glucose absorption and food intake and causes weight reduction.

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