Block 3 Pharm
Terms
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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
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Block muscarinic receptors in the striatum, so ACh cannot bind.
This balances the cholinergic/dopaminergic activity in the basal ganglia - trihexyphenidyl
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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
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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
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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
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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
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Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening - diazepam
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Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening - methocarbamol
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Muscle Relaxants
Facilitate GABAA receptors by ↑ frequency of Cl- channel opening - hydrocodone
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Opioid Analgesics
μ-opioid receptor agonist - morphine, hydrocodone, fentanyl, meperidine
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Opioid Analgesics
μ-opioid receptor agonist - amitriptyline
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anti-neuritic pain relievers
Promote serotonergic and noradrenergic neurotransmission by inhibiting the reuptake of the neurotransmitter—helps to produce antinociceptive states - imipramine
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anti-neuritic pain relievers
Promote serotonergic and noradrenergic neurotransmission by inhibiting the reuptake of the neurotransmitter—helps to produce antinociceptive states - Premarin
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• 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
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⬢ 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
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• Second generation heterocyclic that selectively inhibits serotonin uptake
• Clinical uses—depression - Baclofen
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• 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
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• 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
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MS:
Downregulates MHC expression.
Inhibits proinflammatory cytokines
Increases regulatory cytokines
Inhibits T-cell proliferation - Glatiramer acetate (copaxone)
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MS: reduces attack rate, severity
Binds MHC molecules, alters balance between pro and regulatory cytokines - Natalizumab
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MS:
inhibits attachment of tCells to endothelial cells, preventing BBB crossing. - Mitoxantrone hydrochloride
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MS:
Antineoplastic, interferes with RNA synthesis, inhibits DNA repair. - Azathioprine
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MS:
Immunosupressant interferes with nucleic acid synthesis during S phase. Decreases relapse rate. - Methotrexate
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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
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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
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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
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selective estrogen receptor modulators (SERMS)
breast cancer - raloxifene
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selective estrogen receptor modulators (SERMS)
breast cancer - mestranol
- Estrogen: suppresses ovulation
- etridronate/risedronate/alendronate/pamidronate
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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
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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
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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
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Synthroid
Primary and secondary hypothyroidism is treated by giving T4 - glucagon injection
- Emergency treatment: diabetic becomes unconsciousness - hypoglycemia treatment.
- tolbutamide
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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
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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 PPARï§ 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.