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468 Cards in this Set
- Front
- Back
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asthma
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chronic inflammatory disorder of the airways
involves complex interaxn between many cells and inflammatory mediators that result in inflammation,obstruction , inc airway responsiveness and episodic asthma sx |
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precipitating factors of an acute ashtma exacerbation
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allergens
occupational exposures viral resp tract infxn exercise emotions exposure to irritants environmental exposures drugs |
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allergens
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pollen
house dust mite animal dander mold cockroach food |
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occupational exposures
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chemical irritants
flour wood textile dusts |
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emotions
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anxiety
stress hard laughter crying |
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exposure to irritants
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strong odors
chemical fumes |
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environmental exposure
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weather changes
cold air sulfur dioxide cigarette smoke |
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problematic drugs
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aspirin
nsaid b adrenergic blkers bethanechol meds/food containing tartrazine, sulfites and other preservatives |
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characteristics of asthma
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hypertrophy of smooth muscle
airways containing plugs consisting of inflammatory cells and their debris, proteins and mucus inflammatory cellular infiltrate w/ vasodilation, denuded airway epithelium and microvascular leakage vasodilation of the vasculature denuded airway epithelium microvascular leakage collagen deposition in basement membranes |
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inflammatory cells
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mast cells
eoxinophils activated T cells macrophages epithelial cells |
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axn of inflammatory cells
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secrete mediators and influnce the airways directly or via neural mechanisms
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severe airway obstruction
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bronchoconstriction
airway wall edema mucus plug formation airway remodeling smooth muscle hypertrophy hyperplasia |
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airway obstruction
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reduces ventilation to some lung regions
causes a ventilation/persulsion imbalance that leads to hypoxemia |
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hypoxemia
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reduction in partial pressure of arterila oxugen(PaO2)observed in moderate to severe exacerbations
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hyperresponsiveness
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exaggerated response to certain stimuli
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primary mechanism resp for airway responsiveness
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inc levels of inflam mediators
infiltration by inflam cells |
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resp for altered mucociliary fxn
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inflammatory cells
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acute inflammation
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early recruitment of cells to the airway
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subacute inflam
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recruited and resident cell activation -> persistent inflam
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chronic inflam
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persistent cell damage and ongoing repair -> airway abnormalities and may become permanent
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100mg/dL of alcohol
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Ultrastructural heart damage
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200-300 mg/dL
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Blood alcohol levels that cause emesis
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5,000-10,000 molecules
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New synthesized drugs introduced
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Acetylation
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Phase 2 metabolic rxn
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Acetylcholine
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Not used due to rapid hydrolysis and lack of specificity
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Acetylcholine vasodilator due to
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Release of endothelial relaxing factor
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Activation of G proteins and 2nd messengers
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Acetylcholine (muscarinic rec),
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Admin of sof bicarbonate
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Increase the excretion of aspirin in the urine
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Affinity
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Drug-rec interaxn is reciprocal of equilibrium dissociation constant
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Akathisia
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Restlessness
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Aldehyde dehydrogenase
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Primary pathway for ethanol metabolism
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Alpha 1
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Vasoconstriction
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Alpha 2
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Inhibition of norepi release
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Alpha adrenergic blocking agents
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Convert EPINEPHRINE vasoconstrictor to vasodilator
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Alter rate of metabolism by CYP450
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Charcoal-broiled foods, cigarette smoke, grapefruit juice
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Amantadine
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Antiviral – effectiveness in parkinsonism
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Amitriptyline
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Sedative and antimuscarinic action
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Animal testing
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Initial evaluation of new drug toxicity
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Antagonist
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Binds to rec site but does not produce any direct effect
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Anticholinergic agents
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Hot, dry skin, delirium
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Apomorphine
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Induce vomiting
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Atracurium
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Broken down spontaneously to form laudanosine (quarternary acid)
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B agonist in bronchial asthma
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Manage acute contraction of airway smooth muscle
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B blocking agents in htn
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Combo of inhibition of cardiac output and renin release
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B2 receptor
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Smooth muscle relaxation
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B3 receptor
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Primary location is on the lipocytes
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Benzocaine
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Topical use only
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Beta 2
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Bronchodilation
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Beta agonist with ISA
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Potential to have less depressant effects on the heart
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Beta carbolines
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Inverse agonist
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Bethanechol
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Increase tone of urinary retention & not hydrolysed by cholinesterases
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Botulinum toxin
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Inhibits release of acetylcholine from cholinergic fibers
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Bretylium
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Inhibits morepi release from adrenergic nerve endings
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Bromocriptine
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Hyperprolactinemia
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Bupivacaine
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Long acting and potent amide type local anesthetic
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BZ1
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Zaleplon and zolpidem have selectivity
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Caffeine
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Most common CNS stimulation
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Cardioselectivity
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Bronchial asthma
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Catalyzed by microsomal mixed fxn oxidase system
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hydrolyses, oxidations, reduction
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CBZ
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Frequency repetitive firing of neurons
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Chemical antagonism
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Protamine/heparin
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Clozapine
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Antipsychotic, bone marrow suppression or agrnaulocytosis ,least likely to produce extrapyrimidal side effects
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Cocaine
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No vasoconstrictor is needed
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Commonly affected by chirality
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Ability of the drug to activates its rec
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Comprehensive drug abuse prevention and and control act
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Set controls on habit forming drugs manufacturing
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COMT
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Leads to prdxn of normetanephrine
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Covalent bonds
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Least likely to contribute to very selective drug action
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D1 receptor
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Renal vasodilation
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D2
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Estrapyramidal side eff of antipsychotic
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Density of medium
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Not included in the calculation flux
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Dextromethorphan
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Cough suppressant, no opiod dependence
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Diazepam
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Most effective in stopping attacks of gen tonic-clonic status epilepticus
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Direct binding to and inhibition of an enzyme catalyzing a key metabolic reaction
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Methotrexate
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Dopamine
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Low conc = increase blood flow to kidney
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Dopamine beta hydroxylase
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Found in effluent ff adrenergic nerve stimulation
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Dosing rate
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Clearance x target conc
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Durham-Humprey
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Power to FDA to determine w/c drugs sold without Rx
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Effect of irreversible antagonist on an agonist conc-response curve
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It will not affect the EC50 but will decrease the max effect
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Effect of reversible ,competitive antagonist on an agonist conc-effect curve
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Increase the EC50 but not change the max effect
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Endomorphin 1
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Peptide –greatest affinity for mu opiod receptors
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Endozepines
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Naturally occurring molecule that has affinity for benzodiazepine receptor
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Enzyme inducers
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Benzopyrene, Phenobarbital, phenytoin, rifampin
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Epinephrine
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Treat acute hypersensitivity rxn to drugs
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Esmolol
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In OR develop arr- quick eff-duration of action
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Ester local anes
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Responsible for allergic response
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Ethosuximide
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Absence seizures
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Extraction ratio
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Hepatic clearance / hepatic blood flow
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F
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Absorption x (1-extraction ratio)
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Fentanyl
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Very potent analgesic patch
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Fetal alcohol syndrome
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Flattened face
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Flumazenil
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Benzodiazepine antagonist
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Fluvoxamine
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No sedative and antimuscarinic action
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Food, drug and cosmetic act of 1938
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Required that all new drugs be safe
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Gabapentin
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Excreted in urine unchanged
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Glaucoma
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Timolol
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Glucocorticoids
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Inhibits reuptake of norepi into extraneuronal sites
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Glutamate
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Neurotransmitter aasoc w/Parkinson
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Halothane
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Depresses the heart rate during anesthesia
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Hemicholinium
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Blocks reuptake of choline into cholinergic fibers
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Henderson-hasselbach equation
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Calculate degree of ionization of weak acids and bases
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Hyperbolic
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Relationship between drug conc and eff
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Hypnotic agents
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Produce restful sleep
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Idiosyncratic response
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Infrequently observed in most pt’s
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Induce CYP450
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Glucocorticoids, macrolide abx, Phenobarbital, polycyclic aaromatic hydrocarbons
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Inhibition of CYP 450 competitive inhibition
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Cimetidine and ketoconazole
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Intrinsic sympathomimetic activity
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Pt forgets to take dose
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IV barbiturate
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Cause tissue necrosis ff extravasation
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Kefauver-Harris
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New drugs proof of efficacy
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Levodopa
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Prolonged w/ admin of COMT inhibitor
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Local anesthetic action
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Must have lipophilicity & hydrophilicity
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Loperamide
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Diarrhea
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Lorazepam
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Least likely to cause enzyme induction
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Maintenance dose
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Dosing rate x dosing interval
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MAO
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Inhibition leads to dangerous increases in BP when fermented foods are taken
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MAO – fermented foods
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Antidepressant most dangerous
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MAOI
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Phenelzine
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Methacholine
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Used for cardiovascular eff
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Methadone
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Opiod dependence
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Methanol intoxication management
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Folic acid,IV ethanol,alkalinization w/ bicarbonate, hemodialysis
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Metyrosine
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Inhibits rate limiting enzyme resp for norepi synthesis
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Midazolam
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Flumazenil
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Mirtazapine
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Unique 3rd gen , does not block the amine pump for noreepi or serotonin
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Mixed function oxidase
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CYP2B1
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Morphine
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Most appropriate for minimal circulatory reserve
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Muscarinic
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Bradycardia
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Muscarinic agonist
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Asthma, coronary insufficiency, peptic ulcer
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Muscarinic M1 receptor
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Activation of phosphoinositide pathway in CNS neurons and sympathetic postganglionic neuron
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Muscarinic receptors
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Contraction of vascular smooth muscle
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naltrexone
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Induce withdrawal, pinpoint pupils, respiratory depression
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Nicotinic
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Release of adrenal catecholamines
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Nicotinic agonist
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Stimulate skeletal muscle and ganglionic sites
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Nicotinic Nm receptor
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Skeletal muscle contraction
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Nicotinic Nn receptor
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Ganglionic stimulation
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Nitrous oxide
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Shortest induction time
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nonCatecholamines Vs catecholamines
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Adv noncatecholamines= longer duration of action in cns
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Nongenetic factors for individual variation in drug distribution, biotransformation and elimination
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Age , circadian rhythm, liver fxn, sex
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Opening or closing of ligand gated ion channels
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GABA, Acetylcholine (nicotinic rec)
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Oral maintenance dose
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Dosing rate x dosing interval
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Orphan drug amendments of 1983
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Incentives for development of drug that treat dz that occur less than 200,000 pt’s
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Pancuronium
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Moderate block of cardiac muscarinic receptor, no effect on ganglia and no tendency to cause release of histamine
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Phase 1
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Small # of healthy volunteers (25-50)
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Phase 1 depolarizing blockade
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Tetanus producing nerve stimulation
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Phase 2
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Patients with the target disease 4 efficacy
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Phase 4
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Large # after approved NDA
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Phenothiazine
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Orthostatic hypotension
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Phenoxybenzamine
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Forms ethyeneimonium ion
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Phenylcyclidine (PCP)
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Trmt of hallucinogenic drug overdose
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Phenylephrine
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Increase in peripheral resistance w/out cardiac stimulation
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Phenylethanolamine n-methyltransferasse
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Responsible 4 synthesis of epinephrine
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Phenytoin
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Interference with ion conductance thru Na channels
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Phosphate
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Administered w/ ethanol intoxication
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Physical dependence
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w/drawal results in physiologic changes
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Physiological antagonism
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Insulin/glucocorticoids
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Potency
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Ed50
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Pramipexole
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Dopamine agonist – non ergot
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Procaine
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Ester type compd –shortest duration of action
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Progressive depression of CNS
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Sedation - hypnosis - anesthesia - coma –death
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Pseudo zero order
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Ethanol eliminated from the body
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Pure food and drug act of 1906
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Prohibited mislabeling and adulteration of drugs
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Quantal dose-effect curve
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Conversion of cardiac arrhy to normal rhythms in a pt population
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Quarteynary
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Permanently charged amine
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Rapacuronium
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Most rapid onset neuromuscular
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Receptor phosphorylation
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Desensitization of b adrenoeceptor in continue presence of agonist
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Regulation of gene transcription by intracellular receptors
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Glucocorticoids, Thyroid hormones, Vitamin D
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Reserpine
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Leads to loss of granular storage of norepinephrine
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Sedative agents
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Produce reduction of anxiety
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Selectivity
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Comparing the ED50 for different responses to the same drug in vivo
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Selegiline
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Inhibits metabolism of dopamine
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Smooth endoplasmic reticulum
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Most CYP450 enzymes located
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SSRI
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Fluoxetine
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Stage 2
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Breath holding, retching, irregular respiration
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Steady state
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First dose / 0.5
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Succinylcholine
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Shortest duration- depolarization type
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Synaptobrevin
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Cellular protein promotes fusion of vesicular membrane
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Tachyphylaxis
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Rapid diminution of a tissues sensitivity to a drug after administration
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TCA
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Imipramine
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TCA excessive quantity
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Death
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Tetracaine
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Ester local anesthetic high potency, long duration of action
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Timolol
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Reduce MI mortality
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TPA
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Biotech and cloning genes ex
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Transport by diffusion across membranes
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Most dependent on the ability of a drug to dissolve in a lipid membrane
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Transport proteins
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Macromolecule targeted by cardioactive dig glycosides to produce eff on heart
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Trazodone
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Considerable sedative action , no antimuscatinic side eff
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Treatment of alcohol withdrawal
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Maintain K and MG balance,
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Tubocurarine
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Nondepolarizing neuromuscular blocker
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Valproate
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Absence, complex partial, generalized tonic-clonic, simple partial
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Vesamicol
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Alters storage of acetylcholine in dense core vesicles
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2ndary hypercholesterolemia
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Early nephrosis
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Abciximab, eptifibatide, tirofiban
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Reduces platelet aggregation by bunding to the platelet IIb/IIIa receptor complex
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ACE
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Altered taste
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ADHD
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Interference w/ hormone receptors
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Alpha receptor of vessels
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Nonselective drug action leads to excessive tachycardia
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Aminocaproic acid
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Inhibitor of fibrinolysis
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Amiodarone
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Antiarr broad spectrum activity
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Amiodarone
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Markedly prolong action potential duration
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Angiotensin 1
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Enzymatic action of renin
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Antiatherogenic
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HDL
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Aspirin
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Irreversibly acetylates cyclooxygenase=> inhibition of the synthesis of thromboxane A2
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Atherogenic
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VLDL, IDL, LDL
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Atrial natriuretic peptide
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Regulation of Na excretion
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B receptors of juxtaglomerular cells
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Hypotensive action – propranolol
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Blue Monday
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Throbbing headaches caused by loss of tolerance
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BPH
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Avoid K sparing diuretics
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Bradykinin
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Vasodilator axn-arteries ;contracts veins
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Bretylium
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Cause initial tachycardia
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Calcium overload
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Digoxin induced arrhythmias
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Cardiac inotropic actions of digoxin
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Consequence of Na/K aTPase inhibition
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Ccb+ tachy
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Verapamil
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CHF = digoxin
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Avoid high intake of sodium
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Clopidrogel
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Blocks adenosine diphosphate receptor on platelets =>reduce platelet aggregation
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Colestipol
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Inhibits absorption of cholesterol bile acids
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Digoxin
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Eliminated in the kidney
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Dihydropyridine – nimodopine, nifedipine, nicardipine
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More selective vasodilator than verapamil (phenylalkylamine)
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Diuresis
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Elimination of urine volume
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ECG induced digoxin
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Increasing PR interval
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Effect of warfarin
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Reversed by vitamin K
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Endothelin
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Vasoactive peptide – iv injection causes vasodilation followed by vasoconstriction
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Furosemide
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Altered hearing
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Gemfibrozil
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Elevated triglyceride levels
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Half life of digoxin
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Requires 1 week to stabilize pt w/ maintenance dose
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Isosorbide dinitrate
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Orally effective form of nitrovasodilator
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Kidney tubules
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African American respond better
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Lepirudin
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Inactivates fibrin bound thrombin in thrombi
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Lidocaine
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Shortens the duration of action potential
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Low MW heparin
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inhibits factor X
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Magnesium
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Counter the cardiotoxicity of digoxin
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Metoprolol
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Inhibits catecholamine-induced arr
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Niacin
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Reduced HDL levels
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Nsaids inhibit
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Aldosterone antagonists , carbonic anhydrase inhibitor, thiazides, triamterene
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NTG
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Relaxes smooth muscle
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Omega 3 fatty acid ingestion
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Lower triglycerides
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Organic nitrites
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Effective in erectile dysfunction
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Pindolol
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Partial agonist, ISA
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Procainamide
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Renal failure, torsade de pointes
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Quinidine
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Blocks Na channels and increases duration of the action potential
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Re-entry phenomena
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Abnormalities in cardiac conduction that give rise to abnormal cardiac rhythms
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Rifampin
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Decrease anticoagulant effect of warfarin by inducing hepatic enzymes that transform the anticoagulant in the body
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Simvastatin and lovastatin
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Must be converted in GI tract to an active compound
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Spironolactone
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Hyperkalemia
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Streptokinase
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Proactivator plasminogen
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Sympathetic nerve terminals
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Antihypertensive action of reserpine and guanethidine
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Unfractionated heparin
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Activated partial thromboplastin time
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Unstable angina
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Decreased platelet aggregation
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Vasoactive intestinal peptide
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Modulator, relax airway & vascular smooth muscle
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Vasomotor center – clonidine
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Lower BP
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Vasopressin
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Increase water absorption
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Verapamil
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Dependent on Calcium channel blockade
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Warfarin
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Blocks gamma carboxylation of glutamate residues in factors 2,7,9,10
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Iron deficiency
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Chronic anemia
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Iron dextran
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Appropriate for parenteral admin
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Hydroxycobalamin
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Treat pernicious anemia
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Erythropoietin
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Anemia caused by renal failure
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Respond to G-CSF granulocyte colony stimulating factor
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Neutropenia caused by cancer chemotherapy
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Folic acid
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Provides a cofactor to produce deoxythymidylate
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Rhodopsin
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11-cis-retinal
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Hypervitaminosis A
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Erythematous dermatitis, neurologic sx, pain and tenderness of bones, papilledema
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Vitamin K 1
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Prevent hypoprothrombinemia newborn
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Vitamin D
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Hypocalcemia asso chronic renal failure
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Hypervitaminosis D
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Elevated 25-hydroxyvitamin D
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Hydroxylation of 1 carbon only
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Conversion Vit D3 to calcitriol
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Effect of PTH in kidney
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Decrease excretion of Ca but increase excretion of phosphate
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Calcitriol effect
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Bone/intestine- increase Ca & phosphate
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Etidronate
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Osteomalacia not seen in fosamax
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Alendronate
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Increase bone density w/ osteoporosis
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Hypercalcemia
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Calcitonin, etidronate, furosemide, gallium nitrate
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Oxytocin
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Activation of receptors coupled to a G protein which activates calcium phosphoinositide signaling pathway
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Leuprolide
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Synthetic analog of GnRH
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Order of potency
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T3>T4> reverse T3
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<1%
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Free circulating thyroid hormone
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Influence oral absorption of levothyroxine
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Al containing antacids, food, iron, sucralfate
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Thyroid hormones action
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Activate receptors in cell nucleus, modulating formation of mRNA coding for certain proteins
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Levothyroxin (T4)
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Agent of choice for thyroid replacement
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Thioamides
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Methimazole and PPU
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Methimazole
|
Qd dosing – mild to moderate hyperthyroidism – accumulated by thyroid gland; onset = 3-4 weeks
|
|
|
Propylthiouracil
|
Inhibits peroxidase catalyzed reaction to block iodine organification in thyroid gland
|
|
|
Estrogens
|
Increase binding of thyroxine by TBG
|
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Potassium perchlorate
|
Antithyroid action – competitive inhibition of uptake of iodide into thyroid gland
|
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|
Iodide
|
Inhibition of release of preformed thyroid hormone from the thyroid gland
|
|
|
Neutrophils
|
Leukocyte increases blood conc after single dose of short acting glucocorticoid
|
|
|
Glucocorticoids
|
Interfere with Vit D action
|
|
|
Fludrocortisone
|
Synthetic steroid greatest salt-retaining activity
|
|
|
Dexamethasone
|
Steroid longest duration of action
|
|
|
Betamethasone
|
OB to prevent incidence of respiratory distress syndrome in infants premature delivery
|
|
|
Hydrocortisone
|
Corticosteroid cause Na and fluid retention and loss of potassium
|
|
|
Thin emaciated facial features
|
Least likely to occur after 2 weeks of glucocorticoid admin
|
|
|
Complication of long term glucocorticoid therapy
|
Muscle wasting, osteoporosis, peptic ulcers , thinning of the skin
|
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|
Progesterone receptors
|
Stimulated by estrogens
|
|
|
Estrogen admin
|
Fertility least likely to occur
|
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|
Progestin
|
Reduce risk of endometrial cancer
|
|
|
Effects of HRT in postmenopausal
|
Reduction of osteoporosis, relief of atropic vaginitis,relief of hot flashes, relief of excessive sweating
|
|
|
Osteoporosis risk factor
|
Caucasian,inactive lifestyle. Smoking
|
|
|
17 alpha alkylated androgen
|
Side effect in liver
|
|
|
Half life of circulating insulin
|
3-5 minutes
|
|
|
Insulin on liver
|
Inhibits conversion of amino acid to glucose
|
|
|
Ultralent insulin
|
Longest duration of action
|
|
|
Hypoglycemia
|
Most common complication of insulin
|
|
|
Sulfonyurea
|
Inhibit efflux of K ions thry ATP sensitive K channels in pancreatic B cell
|
|
|
Rosiglitazone and pioglitazone
|
Act as agonists for nucler PPAR -> activates insulin-responsive genes
|
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|
Acarbose and Miglitol
|
Inhibit alpha glucosidase activity in the intestine
|
|
|
Repaglinide and nateglinide
|
Release insulin from pancreas
|
|
|
2nd gen sulfonylurea
|
Glyburide, glimepride, glipizide
|
|
|
Glyburide
|
Hypoglycemia
|
|
|
Repaglinide
|
Control postprandial glucose excursion
|
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|
Glucose
|
Precipitate symptoms of thiamine deficiency in marginally nourished pt’s
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|
|
Nicotinic acid
|
Prophylaxis & trmt of pellagra
|
|
|
Oxacillin
|
B lactam abx most resistant to staphylococcal beta lactamases
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Ampicillin
|
Improved activify against gram –ive rods
|
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|
Transpeptidation reaction
|
B lactam abx – bactericidal action
|
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|
Induction of transpeptidase
|
Least likely to contribute to bacterial resistance to PCN
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Methicillin
|
Most nephrotoxic
|
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Amoxicillin
|
Cleared by kidneys lowere dose in renally compromised function
|
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|
Beta lactamase inhibitor
|
Clavulanic acid
|
|
|
PCN
|
Cross-reacting and cross sensitizing
|
|
|
Cefaclor
|
Most susceptible to hydrolysis by beta lactamases
|
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|
Ceftriaxone
|
3rd gen cepha achieves conc in the CSF sufficient to inhibit most pathogens
|
|
|
Staphylococcus bacteria
|
Beta lactamase are most effective against beta lactamases produced by
|
|
|
Erythromycin abx axn
|
Ribosomal protein biosynthesis
|
|
|
Interfere with TCN absorption
|
Alkalin pH,antacids,dairy products, divalent cations
|
|
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Doxycycline
|
Most suitable for renal insufficient pt
|
|
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Minocycline
|
Tcn longest duration of action
|
|
|
TCN admin during pregnancy
|
Affect bone tissue
|
|
|
Clarithromycin
|
Better acid stability & oral absorption than erythromycin
|
|
|
Cross resistance
|
Linezolid VS clinda, ery,quinupristin-dalfopristin
|
|
|
Ribosomal protein biosynthesis
|
Antibiotic activity of type B streptogramins due to blockade
|
|
|
Chloramphenicol
|
Greatest liability for producing toxic effects on the bone marrow
|
|
|
Aminoglycosides abx
|
Useful with aerobic gram(-)
|
|
|
Streptomycin
|
Vestibular dysfunction – toxic eff
|
|
|
Neomycin
|
Least absorbed from GI tract after oral
|
|
|
Tobramycin
|
Most similar to gentamicin
|
|
|
Sulfonamide chemical structure
|
Most similar to PABA
|
|
|
Sulfadoxine
|
Sulfonamide with the longest duration of action
|
|
|
Sodium bicarbonate
|
Useful in treating nephrotoxicity caused by sulfadiazine
|
|
|
Trimethoprim
|
Given therapeutic doses concentrate in the prostatic fluid and vaginal fluid
|
|
|
Quinolone
|
Synthetic fluorinated analogs of nalidixic acid
|
|
|
Cipro
|
Antimicrobial axn –topoisomerase II /IV
|
|
|
Fluoroquinolone
|
Most common N/V , diarrhea
|
|
|
Pyridoxine
|
Reverse peripheral neuropathy caused by isoniazid
|
|
|
Mutation preventing binding of rifampin to RNA polymerase
|
Main cause of resistance of mycobacteria to rifampin
|
|
|
Ethambutol
|
Visual disturbance
|
|
|
Amphotericin B
|
Renal toxicity
|
|
|
Flucytosine
|
Antifungal activity – inhibition of DNA and RNA synthesis
|
|
|
Terbinafine
|
Antifungal activity – inhibition of squalene epoxidase
|
|
|
DNA synthesis
|
Viral replication targeted by Acyclovir
|
|
|
Alteration of thymidine kinase
|
Resistance to acyclovir develops
|
|
|
Cidofovir IV
|
Nephrotoxicity
|
|
|
Inhibition of protein synthesis
|
Fomiversen inhibits virus replication by
|
|
|
Nucleoside reverse transcriptase inhibitor
|
Zidovudine
|
|
|
Didanosine
|
Pancreatitis
|
|
|
Zalcitabine
|
Peripheral neuropathy
|
|
|
Indinavir
|
Protease inhibitor – highest CSF penetration
|
|
|
Ritonavir + saquinavir
|
Increase the conc of saquinavir reaching the systemic circulation
|
|
|
Metronidazole
|
Most effective – extraintestinal infection by Entamoeba histolytica
|
|
|
Bactrim
|
P carinii pneumonia
|
|
|
Primaquine
|
Doc for eradication of dormant hepatic stages of Plasmodium vivax and ovale
|
|
|
Pyrimethamine
|
Antimalarial plasmodial dihydrofolate reductase
|
|
|
Alkylating agents
|
Cell cycle nonspecific
|
|
|
P glycoprotein
|
Cellular glycoprotein that transports foreign molecules
|
|
|
Reduction of WBC
|
Major toxicity produced by alkylating
|
|
|
Plant alkaloids
|
Cell cycle specific anticancer drugs
|
|
|
Methotrexate
|
Intracellular formation of polyglutamate
|
|
|
Chlorambucil
|
Cause cell death
|
|
|
Cytarabine
|
Converted in the body to a metabolite that blocks DNA synthesis by competitive inhibition of DNA polymerase
|
|
|
Vinblastine
|
Arrest in metaphase
|
|
|
Etoposide
|
Block progression thru cell cycle by inhibition of topoisomerase II
|
|
|
Dactinomycin
|
Anticancer drug inhibits DNA dependent RNA synthesis mainly as a result of its intercalation between adjacent guanine-cytosine base pairs in double stranded DNA
|
|
|
Immunosuppression in transplant pt’s
|
Antiproliferative/antimetabolic agents,
|
|
|
Cyclosporine
|
Binds to cyclophilin, => inhibit calcineurin in T lymphocytes
|
|
|
Sirolimus
|
Binds to intracellular protein FK506 binding protein 12
|
|
|
Tacrolimus
|
Binds to FKBP-12
|
|
|
Glucocorticoids
|
Admin prior to treatment with muromonab-CD3 to suppress cytokine release syndrome
|
|
|
Infliximab
|
Chimeric antitumor necrosis factor-alpha monoclonal antibody
|
|
|
CD154
|
Molecule that downregulates immune responses
|
|
|
Levamisole
|
Restore depressed immune function of B and T lymphocytes, monocytes and macrophages
|
|
|
Thalidomide
|
Immune modulating agents carries the strongest warning against OB
|
|
|
Human recombinant IL-2
|
Linked to serious cardiovascular toxicity due to capillary leak syndrome
|
|
|
Interferon gamma 1B
|
Most effective in causing activation of phagocytes and production of oxygen metabolites that are toxic to microorganisms
|
|
|
1-3 months
|
Protection from passive immunization using an immune globulin prep typically last
|
|
|
Carbon monoxide
|
Most abundant pollutant
|
|
|
Paraquat
|
Toxicity due to free radicals
|
|
|
Nitrogen oxide
|
Inhaled agents where farmers or workers who deal with silage can be poisoned
|
|
|
Ozone
|
Bluish irritant gas
|
|
|
Pyrethrum
|
Botanical poisoning, seizures, allergic response => contact dermatitis
|
|
|
Nicotine
|
Salt not readily absorbed thru the skin but the base is
|
|
|
Halogenated hydrocarbon
|
Assoc liver, renal, cardiac toxicity
|
|
|
Glucagons
|
Treat b adrenergic blocker intoxication
|
|
|
Organophosphate insecticides
|
Dumbels
|
|
|
Beta antagonists
|
Theophyline intoxication
|
|
|
Tricyclic drug overdose
|
Admin norepi to raise blood pressure
|
|
|
Edetate calcium disodium
|
Lead intoxication
|
|
|
Penicillamine
|
1st line of treatment for Wilson’s dz
|
|
|
Deferoxime
|
Iron poisoning
|
|
|
British anti-lewisite
|
Dimercaprol
|
|
|
oxygen
|
Carbon monoxide poisoning
|
|
|
Ethanol
|
Methanol toxicity
|
|
|
Naloxone
|
Opioid overdose
|
|
|
Pralidoxime
|
Early stages of organophosphate intoxication
|
|
|
Acetylcysteine
|
Acetaminophen toxicity
|
|
|
Cathartics
|
Enhance elimination of iron tabs, enteric coated agents, illicit drug packages
|
|
|
Emesis
|
Should be avoided in pt;s who have ingested a petroleum distillate
|
|
|
Activated charcoal
|
Eliminates toxic compound- gut dialysis
|
|
|
Cyclosporine
|
RA, DMARD (disease modifying antirheumatic drug
|
|
|
Allopurinol,
|
Decrease formation of uric acid by inhibiting xanthine oxidase
|
|
|
Colchicines
|
Discontinue due to abdominal pain/diarrhea
|
|
|
Probenecid
|
Organic acid inhibit excretion of PCN
|
|
|
Indomethacin
|
Initial trmt of gout as prostaclandin syntase inhibitor
|
|
|
|
|
|
|
GASTROINTESTINAL PHARMACOLOGY
|
|
|
|
PPI
|
Prodrugs
|
|
|
Suppression of nocturnal acid secretion
|
Most important determinant of rate of healing of duodenal ulcer
|
|
|
Chemoreceptor trigger zone
|
Antiemetic agent , inhibit chemically induced N/V
|
|
|
Metoclopramide
|
Restore motility
|
|
|
Cimetidine
|
Alter drug metabolism
|
|
|
Aluminum based antacid
|
Constipation
|
|
|
Cascara
|
Laxation when stimulation of peristalsis is desired
|
|
|
Mineral oil
|
Stool softener
|
|
|
Sulfasalazine
|
Inflammatory bowel disease
|
|
|
Methylcellulose
|
Hydrophilic colloid used a laxative
|
|
|
Infliximab
|
Inhibitor to tumor necrosis factor alpha for management of Crohns dz
|
|
|
Bismuth subsalicylate
|
Mucosal protective agents
|
|
|
Bronchial asthma
|
Nonspecific bronchial hyperreactivity
|
|
|
Controller drugs
|
Mgmt of bronchial asthma
|
|
|
Inhaled corticosteroid
|
Airway inflammation is linked to increase airway responsiveness
|
|
|
Aminophylline
|
Methylxanthine
|
|
|
Methylxanthine action
|
Inhibition of adenosine receptors
|
|
|
Theophylline
|
Requires periodic monitoring of plasma levels
|
|
|
Cromolyn
|
Inhibition of delayed chloride channels
|
|
|
Nedocromil
|
Administered prophylactically
|
|
|
Ipratropium
|
Quarternary amine
|
|
|
Corticosteroids adv eff
|
Adrenal suppression, hoarseness, oral candidiasis, osteoporosis
|
|
|
Physiologic inhibition
|
Occurs upon Epinephrine admin
|
|
|
H2 receptor
|
Similar to serotonin
|
|
|
Sleepiness
|
Penetration of antihistamines into CNS
|
|
|
Fexofenadine
|
Nonsedating
|
|
|
Promethazine
|
Antiemetic
|
|
|
Melatonin
|
Regularize sleep patterns
|
|
|
5HT2 receptors
|
Stimulation = intense CNS vasoconstrictive action of ergot alkaloids
|
|
|
Epinephrine reversal
|
Vasoconstriction of ergot alkaloids leads to gangrene
|
|
|
Guinea pig
|
Hypersensitive to histamine
|
|
|
Motion sickness
|
Ephedrine + H1 antagonist
|
|
|
Anticholinergic action of benztropine
|
Parkinson like tremor antagonized for antipsychotic agents
|
|
|
|
|
|
|
|
At this point, initiating agents is most likely methacholine, IgE is binding to mast cells at this time.
|
|
|
Cromakalim
|
activator of K channels
|
|
|
Zafirlukast
|
Inhibitor of leukotriene at receptor level
|
|
|
Prednisone
|
Used in large doses for severe acute episodes of asthma
|
|
|
Zileuton
|
Lipoxygenase inhibitor
|
|
|
Salmeterol
|
Long acting agent of choice for management of nocturnal asthma
|
|
|
Glutathione
|
Limited amt in phase 2 reaction , inability to convert toxic metabolites to inactive products
|
|
|
Pentazocine
|
Produce hallucinations and nightmares
|
|
|
Continuos loss of nigrostiratal neurons
|
Waning of Levodopa therapy Parkinson
|
|
|
Epinephrine
|
Reverse bonchospasm
|
|
|
Vecuronium
|
Eliminated from the body mainly by excretion of unchanged drug or its 3-hydroxy metabolite in bile
|
|
|
S-mephenytoin
|
More slowly metabolized in some individuals due to reduced rate of hydroxylation caused by genetic polymorphism of CYP2C19
|
|
|
Dantrolene
|
Most appropriate for treating the malignant hyperthermia triggered by a combination of general anesthesia and a neuromuscular blocking agent
|
|
|
Dissociative anesthesia
|
Ketamine produces catatonic state with amnesia and analgesia
|
|
|
Flunitrazepam
|
Date rape drug
|
|
|
Furosemide
|
High sodium
|
|
|
Hypothyroidism
|
Radio iodine therapy
|
|
|
Metformin
|
GI disturbances
|
|
|
Iv and smoking
|
Fastest and highest blood levels of cocaine route
|
|
|
Hyperlipidemias
|
Primary chylomicronemia
|
|
|
Antifungal activity axole drugs
|
Inhibition of CYP450
|
|
|
Nevirapine
|
Severe & life threatening skin rashes
|
|
|
Hemolysis
|
Glucose 6 phosphate dehydrogenase deficiency
|
|
|
Acute myelogenous leukemia
|
2nd most frequent malignancy encountered in cancer chemotherapy
|
|
|
Lipocortin
|
Inhibition of the production of prostaglandins and leukotriene in macrophages, monocytes, endothelial cells and fibroblast
|
|
|
Rattlesnake envenomation
|
Managed by large amts of antivenin
|
|
|
H3 receptors
|
Presynaptic
|
