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Pharm 1 - Cholinergics, Adrenergics, Immuno, MSK+Rheum

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gsafsaf's version from 2015-05-23 23:00

Cholinergic drugs

Question Answer
BethanecolDirect muscarinic agonist; treats ileus (post op. usually)
CarbacholDirect muscarinic agonist; treats glaucoma
PilocarpineDirect muscarinic agonist; increases saliva production - treats xerostomia caused by radiation or Sjögren's
NeostigmineIndirect muscarinic agonist; Myasthenia Gravis; post op. and neurogenic ileus; reverses anesthesia NMJ blockade; does NOT penetrate CNS
Pyridastigmine Indirect muscarinic agonist; Long term Myasthenia Gravis treatment; does NOT penetrate CNS
EdrophoniumIndirect muscarinic agonist; "Tensilon Test" to differentiate btwn myasthenic crisis (its administration will improve Sx + MORE cholinesterase inhibitor indicated) vs cholinergic crisis (its administration will NOT improve Sx bc in this case there is excess ACh + LESS cholinesterase inhibitor indicated) vs. Lambert Eaton Myesthenia Gravis (its administration will NOT improve Sx bc not enough ACh is released in the first place); short-acting; does NOT penetrate CNS
PhysostigimineIndirect muscarinic agonist; treats glaucoma; treats atropine overdose; DOES penetrate CNS
DonepezilIndirect muscarinic agonist; Alzheimer's Rx
Galantamine Indirect muscarinic agonist; Alzheimer's Rx
Rivastigmine Indirect muscarinic agonist; Alzheimer's Rx
Atropine Muscarinic antagonist; counters Sx of organophosphate toxicity; treats bradycardia; dilates pupil
HomatropineMuscarinic antagonist; pupil dilation; short acting
TropicamideMuscarinic antagonist; pupil dilation; short acting
CyclopentolateMuscarinic antagonist; pupil dilation; short acting
Benztropine Muscarinic antagonist; treats Parkinson's; lessens side effects of antipsychotics
ScopolamineMuscarinic antagonist; decreases secretions (good for pts on ventilator for ex.); treats motion sickness. [Could use this in pts w Myasethina gravis to reduce side effects of cholinesterase inhibitors in the gut, w/o affecting the action of the cholinesterase inhibitor on skeletal muscle-which uses nicotinic receptors]
IpratropiumMuscarinic antagonist; decreases bronchoconstriction (used in COPD and asthma)
TiotropiumMuscarinic antagonist; decreases bronchoconstriction (used in COPD and asthma)
Oxybutynin Muscarinic antagonist; treats overactive bladder/urge incontinence
TolterodineMuscarinic antagonist; treats overactive bladder/urge incontinence
Darifenacin Muscarinic antagonist; treats overactive bladder/urge incontinence
SolifenacinMuscarinic antagonist; treats overactive bladder/urge incontinence
TrospiumMuscarinic antagonist; treats overactive bladder/urge incontinence
DiphenylhydramineNOT a muscarinic antagonist, but has anticholinergic side effects; H1 blocker
Doxylamine NOT a muscarinic antagonist, but has anticholinergic side effects; H1 blocker
AmantadineNOT a muscarinic antagonist, but has anticholinergic side effects; stimulates dopamine release and blocks dopamine reuptake (Antiviral)
AmitriptylineNOT a muscarinic antagonist, but has anticholinergic side effects (TCA)
ChlorpromazineNOT a muscarinic antagonist, but has anticholinergic side effects (Typical neuroleptic)
ThiordazineNOT a muscarinic antagonist, but has anticholinergic side effects (Typical neuroleptic)
EchothiophateIndirect muscarinic agonist; treats glaucoma
Hemicholiniumcholine uptake inhibitor; no clinical use - a research tool
Vesamicolantagonizes the packaging of ACh into secretory vesicle; research tool
Black widow toxincauses massive release of ACh into synapse --> spastic paralysis
Botulinum toxininhibits ACh release into synapse --> flaccid paralysis
Choline acetylransferaseenzyme that synthesizes ACh from Acetyl CoA and choline. Deficient in Alzheimer's
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Adrenergic

Question Answer
Epinephrine a1, a2, ß1, ß2 agonist; treats anaphylaxis, croup, hypotension
Norepinephrinea2 > a1, ß1 agonist; treats hypotension, septic shock
DopamineD (low dose), ß1, ß2 (medium dose), a1, a2 (high dose) agonist; treats shock
Dobutamineß1 > ß2 agonist; use for heart stress test, cardiogenic shock - positive inotrope
Isoproterenol ß1, ß2 agonist; not really used clinically
Phenylephrine a1 > a2 agonist; use to dilate pupils, nasal decongestant
Albuterol ß2 > ß1 agonist; asthma
Levalbuterolß2 > ß1 agonist; asthma
Salmeterol ß2 > ß1 agonist; asthma
Terbutaline ß2 > ß1 agonist; stops premature uterine contractions, also treats bronchospasm
Clonidinea2 agonist; treats malignant HTN, be careful bc of rebound HTN
Alpha-methyldopaa2 agonist; treats chronic HTN in pregnant women (not gestational HTN)
Prazosinselective a1 blocker; treats men w BPH; S/E of hypotension + reflex tachycardia
Doxazosinselective a1 blocker; treats men w BPH; S/E of hypotension + reflex tachycardia
Terazosinselective a1 blocker; treats men w BPH; S/E of hypotension + reflex tachycardia
TamsulosinVERY selective a1 blocker; only blocks a1 receptor in prostate; treats men w BPH and does NOT cause hypotension/reflex tachycardia
Phenoxybenzaminenonselective a-blocker; treats pheochromocytoma; irreversible a-blocker - so will block catecholamine shower caused by pheochromocytoma
Phentolaminenonselective a-blocker; treats pheochromocytoma
Propanololnonselective ß-blocker; treats HTN
Timololnonselective ß-blocker; treats glaucoma
Nadololnonselective ß-blocker; treats glaucoma
Metoprololselective ß1-blocker; treats HTN
Atenololselective ß1-blocker; treats HTN
Esmololselective ß1-blocker; treats arrhythmia
Pindololweak ß1 and ß2 agonist; so weak it acts as an antagonist; treats HTN (good for pts w HTN + bradycardia)
Acebutololweak ß1 and ß2 agonist; so weak it acts as an antagonist; treats HTN (good for pts w HTN + bradycardia)
Labetalola1 and nonselective ß-blocker used to treat HTN in pregnant women (not gestational HTN) and in eclampsia (alongside other rapid acting antihypertensives + magnesium sulfate)
Amphetamines indirect sympathomimetic; causes release of stored catecholamines; treats narcolepsy, ADHD, obesity
Ephedrineindirect sympathomimetic; causes release of stored catecholamines; treats urinary incontinence, nasal decongestant
Cocaineindirect sympathomimetic; inhibits the uptake of NE; nasal decongestant, anesthesia
Reserpineinhibits conversion of dopamine to NE
Tyraminecatecholamine releasing agent; canNOT cross BBB - nonpyschoactive sympathomimetic effects; hypertensive crisis can result when pt on MAOi ingests tyramine rich foods
Bretyliumblocks NE release from presynaptic cell; anti-arrhytmic
TCAsblock NE reuptake
Catechol-O-methyl transferase (COMT)methylates catecholamines, rendering them inactive
Monoamine oxidase (MAO)oxidizes monoamines such as catecholamines, rendering them inactive
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Immunosuppressants

Question Answer
Binds cyclophilins in the cytosol of T-cellsCyclosporine
Inhibit calcineurin + IL-2Cyclosporine
Rx to prevent transplant rejectionCyclosporine
Autoimmune disorders; Psoriasis, Severe RACyclosporine
S/E - viral infxns, lymphomas, HTN, nephrotoxicityCyclosporine
Constriction of afferent + efferent renal arteriolesCyclosporine
Topical use for EczemaTacrolimus + Pimecrolimus
Bind to FK binding proteinsTacrolimus + Pimecrolimus
Inhibit calcineurin + IL-2Tacrolimus + Pimecrolimus
Rx to prevent transplant rejectionPimecrolimus
S/E Nephrotoxicity + HTNTacrolimus + Pimecrolimus
S/E Neurotoxicity - HA/ParesthesiasTacrolimus
Binds FK binding protein-12Sirolimus
Inhibits mTOR - inhibits T cell proliferationSirolimus
NOT nephrotoxicSirolimus
Precursor of 6-mercaptopurine (6-MP)Azathioprine
Interfere w nucleic acid synthesis (immune cells can't proliferate)Azathioprine
Rx for kidney transplants, autoimmune disordersAzathioprine
Bone marrow suppressionAzathioprine
Metabolized by xanthine oxidase (toxic effects increased by allopurinol)Azathioprine
Inhibits inosine monophosphate (IMP) dehydrogenaseMycophenolate
Inhibits guanine synthesis --> prevents lymphocyte proliferationMycophenolate
Rx for transplantsMycophenolate
Teratogen - causes severe hypoplasia of limbsThalidomide
Suppresses TNF-a production, increases NK cells and IL-2Thalidomide
Rx for erythema nodosum leprosum (Hansen disease), multiple myelomaThalidomide
Rx for seronegative spondyloarthropathies + RAInfliximab + Adalimumab
Monoclonal Abs that bind to TNF-a and render it inactiveInfliximab + Adalimumab
Mimics TNF-a and binds TNF-a receptor to work as antagonistEtanercept
Monoclonal Ab that binds CD20 on B cells to induce complement destruction of those cellsRituximab
Rx for Non-Hodgkin LymphomasRituximab
Monoclonal Ab against IgEOmalizumab
Rx for severe asthma patientsOmalizumab
Monoclonal Ab ag glycoprotein 2B3A receptors on plateletsAbciximab
Inhibits platelet activity - used in patients who have recently undergone angioplastyAbciximab
Monoclonal Ab ag HER2 - used to treat breast cancers that express thisTrastuzumab
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Bone drugs

Question Answer
SmokingAssociated with reduced bone density; increased risk of fracture
AlcoholIncreased fracture risk
GlucocorticoidsInhibition of osteoblasts, enhancement of bone resorption, inhibition of calcium absorption, inhibition of estrogen, increased Ca++ urine loss
PPIs + H2 blockersReduce absorption of Ca++
BisphosphonatesInhibit osteoclasts
BisphosphonatesAssctd w erosive esophagitis
BisphosphonatesAssctd w osteonecrosis of the jaw
TeriparatideRecombinant PTH analogue - stimulates osteoblasts
BisphosphonatesReduced fracture risk in general
TeriparatideDecrease hip fracture rate
TeriparatideIf therapy exceeds two years, increased risk of osteosarcoma
TeriparatideIf given continuously - erodes bones; needs to be given in pulsatile fashion (1x day injection)
TeriparatideAfter therapy discontinued, pt must take a bisphosphonate to maintain mineral density
Testosterone replacementRx for men w osteoporosis
EstrogenShould NOT be given only for osteoporosis, only if there is an additional indication for its use bc of S/E
Selective estrogen receptor modulators (SERMs)Raloxifene
CalcitoninInhibits osteoclasts, Does NOT reduce fracture risk
DenosumabRANK-L inhibitor
Selective estrogen receptor modulators (SERM)sDecrease vertebral fracture rate
EstrogenDecrease hip fracture rate
CalcitoninMiacalcin
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