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Glossary of a and l rev

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asthma
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
precipitating factors of an acute ashtma exacerbation
allergens
occupational exposures
viral resp tract infxn
exercise
emotions
exposure to irritants
environmental exposures
drugs
allergens
pollen
house dust mite
animal dander
mold
cockroach
food
occupational exposures
chemical irritants
flour wood
textile dusts
emotions
anxiety
stress
hard laughter
crying
exposure to irritants
strong odors
chemical
fumes
environmental exposure
weather changes
cold air
sulfur dioxide
cigarette smoke
problematic drugs
aspirin
nsaid
b adrenergic blkers
bethanechol
meds/food containing tartrazine, sulfites and other preservatives
characteristics of asthma
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
inflammatory cells
mast cells
eoxinophils
activated T cells
macrophages
epithelial cells
axn of inflammatory cells
secrete mediators and influnce the airways directly or via neural mechanisms
severe airway obstruction
bronchoconstriction
airway wall edema
mucus plug formation
airway remodeling
smooth muscle hypertrophy
hyperplasia
airway obstruction
reduces ventilation to some lung regions

causes a ventilation/persulsion imbalance that leads to hypoxemia
hypoxemia
reduction in partial pressure of arterila oxugen(PaO2)observed in moderate to severe exacerbations
hyperresponsiveness
exaggerated response to certain stimuli
primary mechanism resp for airway responsiveness
inc levels of inflam mediators
infiltration by inflam cells
resp for altered mucociliary fxn
inflammatory cells
acute inflammation
early recruitment of cells to the airway
subacute inflam
recruited and resident cell activation -> persistent inflam
chronic inflam
persistent cell damage and ongoing repair -> airway abnormalities and may become permanent
100mg/dL of alcohol
Ultrastructural heart damage
200-300 mg/dL
Blood alcohol levels that cause emesis
5,000-10,000 molecules
New synthesized drugs introduced
Acetylation
Phase 2 metabolic rxn
Acetylcholine
Not used due to rapid hydrolysis and lack of specificity
Acetylcholine vasodilator due to
Release of endothelial relaxing factor
Activation of G proteins and 2nd messengers
Acetylcholine (muscarinic rec),
Admin of sof bicarbonate
Increase the excretion of aspirin in the urine
Affinity
Drug-rec interaxn is reciprocal of equilibrium dissociation constant
Akathisia
Restlessness
Aldehyde dehydrogenase
Primary pathway for ethanol metabolism
Alpha 1
Vasoconstriction
Alpha 2
Inhibition of norepi release
Alpha adrenergic blocking agents
Convert EPINEPHRINE vasoconstrictor to vasodilator
Alter rate of metabolism by CYP450
Charcoal-broiled foods, cigarette smoke, grapefruit juice
Amantadine
Antiviral – effectiveness in parkinsonism
Amitriptyline
Sedative and antimuscarinic action
Animal testing
Initial evaluation of new drug toxicity
Antagonist
Binds to rec site but does not produce any direct effect
Anticholinergic agents
Hot, dry skin, delirium
Apomorphine
Induce vomiting
Atracurium
Broken down spontaneously to form laudanosine (quarternary acid)
B agonist in bronchial asthma
Manage acute contraction of airway smooth muscle
B blocking agents in htn
Combo of inhibition of cardiac output and renin release
B2 receptor
Smooth muscle relaxation
B3 receptor
Primary location is on the lipocytes
Benzocaine
Topical use only
Beta 2
Bronchodilation
Beta agonist with ISA
Potential to have less depressant effects on the heart
Beta carbolines
Inverse agonist
Bethanechol
Increase tone of urinary retention & not hydrolysed by cholinesterases
Botulinum toxin
Inhibits release of acetylcholine from cholinergic fibers
Bretylium
Cause initial tachycardia
Bromocriptine
Hyperprolactinemia
Bupivacaine
Long acting and potent amide type local anesthetic
BZ1
Zaleplon and zolpidem have selectivity
Caffeine
Most common CNS stimulation
Cardioselectivity
Bronchial asthma
Catalyzed by microsomal mixed fxn oxidase system
hydrolyses, oxidations, reduction
CBZ
Frequency repetitive firing of neurons
Chemical antagonism
Protamine/heparin
Clozapine
Antipsychotic, bone marrow suppression or agrnaulocytosis ,least likely to produce extrapyrimidal side effects
Cocaine
No vasoconstrictor is needed
Commonly affected by chirality
Ability of the drug to activates its rec
Comprehensive drug abuse prevention and and control act
Set controls on habit forming drugs manufacturing
COMT
Leads to prdxn of normetanephrine
Covalent bonds
Least likely to contribute to very selective drug action
D1 receptor
Renal vasodilation
D2
Estrapyramidal side eff of antipsychotic
Density of medium
Not included in the calculation flux
Dextromethorphan
Cough suppressant, no opiod dependence
Diazepam
Most effective in stopping attacks of gen tonic-clonic status epilepticus
Direct binding to and inhibition of an enzyme catalyzing a key metabolic reaction
Methotrexate
Dopamine
Low conc = increase blood flow to kidney
Dopamine beta hydroxylase
Found in effluent ff adrenergic nerve stimulation
Dosing rate
Clearance x target conc
Durham-Humprey
Power to FDA to determine w/c drugs sold without Rx
Effect of irreversible antagonist on an agonist conc-response curve
It will not affect the EC50 but will decrease the max effect
Effect of reversible ,competitive antagonist on an agonist conc-effect curve
Increase the EC50 but not change the max effect
Endomorphin 1
Peptide –greatest affinity for mu opiod receptors
Endozepines
Naturally occurring molecule that has affinity for benzodiazepine receptor
Enzyme inducers
Benzopyrene, Phenobarbital, phenytoin, rifampin
Epinephrine
Treat acute hypersensitivity rxn to drugs
Esmolol
In OR develop arr- quick eff-duration of action
Ester local anes
Responsible for allergic response
Ethosuximide
Absence seizures
Extraction ratio
Hepatic clearance / hepatic blood flow
F
Absorption x (1-extraction ratio)
Fentanyl
Very potent analgesic patch
Fetal alcohol syndrome
Flattened face
Flumazenil
Benzodiazepine antagonist
Fluvoxamine
No sedative and antimuscarinic action
Food, drug and cosmetic act of 1938
Required that all new drugs be safe
Gabapentin
Excreted in urine unchanged
Glaucoma
Timolol
Glucocorticoids
Inhibits reuptake of norepi into extraneuronal sites
Glutamate
Neurotransmitter aasoc w/Parkinson
Halothane
Depresses the heart rate during anesthesia
Hemicholinium
Blocks reuptake of choline into cholinergic fibers
Henderson-hasselbach equation
Calculate degree of ionization of weak acids and bases
Hyperbolic
Relationship between drug conc and eff
Hypnotic agents
Produce restful sleep
Idiosyncratic response
Infrequently observed in most pt’s
Induce CYP450
Glucocorticoids, macrolide abx, Phenobarbital, polycyclic aaromatic hydrocarbons
Inhibition of CYP 450 competitive inhibition
Cimetidine and ketoconazole
Intrinsic sympathomimetic activity
Pt forgets to take dose
IV barbiturate
Cause tissue necrosis ff extravasation
Kefauver-Harris
New drugs proof of efficacy
Levodopa
Prolonged w/ admin of COMT inhibitor
Local anesthetic action
Must have lipophilicity & hydrophilicity
Loperamide
Diarrhea
Lorazepam
Least likely to cause enzyme induction
Maintenance dose
Dosing rate x dosing interval
MAO
Inhibition leads to dangerous increases in BP when fermented foods are taken
MAO – fermented foods
Antidepressant most dangerous
MAOI
Phenelzine
Methacholine
Used for cardiovascular eff
Methadone
Opiod dependence
Methanol intoxication management
Folic acid,IV ethanol,alkalinization w/ bicarbonate, hemodialysis
Metyrosine
Inhibits rate limiting enzyme resp for norepi synthesis
Midazolam
Flumazenil
Mirtazapine
Unique 3rd gen , does not block the amine pump for noreepi or serotonin
Mixed function oxidase
CYP2B1
Morphine
Most appropriate for minimal circulatory reserve
Muscarinic
Bradycardia
Muscarinic agonist
Asthma, coronary insufficiency, peptic ulcer
Muscarinic M1 receptor
Activation of phosphoinositide pathway in CNS neurons and sympathetic postganglionic neuron
Muscarinic receptors
Contraction of vascular smooth muscle
naltrexone
Induce withdrawal, pinpoint pupils, respiratory depression
Nicotinic
Release of adrenal catecholamines
Nicotinic agonist
Stimulate skeletal muscle and ganglionic sites
Nicotinic Nm receptor
Skeletal muscle contraction
Nicotinic Nn receptor
Ganglionic stimulation
Nitrous oxide
Shortest induction time
nonCatecholamines Vs catecholamines
Adv noncatecholamines= longer duration of action in cns
Nongenetic factors for individual variation in drug distribution, biotransformation and elimination
Age , circadian rhythm, liver fxn, sex
Opening or closing of ligand gated ion channels
GABA, Acetylcholine (nicotinic rec)
Oral maintenance dose
Dosing rate x dosing interval
Orphan drug amendments of 1983
Incentives for development of drug that treat dz that occur less than 200,000 pt’s
Pancuronium
Moderate block of cardiac muscarinic receptor, no effect on ganglia and no tendency to cause release of histamine
Phase 1
Small # of healthy volunteers (25-50)
Phase 1 depolarizing blockade
Tetanus producing nerve stimulation
Phase 2
Patients with the target disease 4 efficacy
Phase 4
Large # after approved NDA
Phenothiazine
Orthostatic hypotension
Phenoxybenzamine
Forms ethyeneimonium ion
Phenylcyclidine (PCP)
Trmt of hallucinogenic drug overdose
Phenylephrine
Increase in peripheral resistance w/out cardiac stimulation
Phenylethanolamine n-methyltransferasse
Responsible 4 synthesis of epinephrine
Phenytoin
Interference with ion conductance thru Na channels
Phosphate
Administered w/ ethanol intoxication
Physical dependence
w/drawal results in physiologic changes
Physiological antagonism
Insulin/glucocorticoids
Potency
Ed50
Pramipexole
Dopamine agonist – non ergot
Procaine
Ester type compd –shortest duration of action
Progressive depression of CNS
Sedation - hypnosis - anesthesia - coma –death
Pseudo zero order
Ethanol eliminated from the body
Pure food and drug act of 1906
Prohibited mislabeling and adulteration of drugs
Quantal dose-effect curve
Conversion of cardiac arrhy to normal rhythms in a pt population
Quarteynary
Permanently charged amine
Rapacuronium
Most rapid onset neuromuscular
Receptor phosphorylation
Desensitization of b adrenoeceptor in continue presence of agonist
Regulation of gene transcription by intracellular receptors
Glucocorticoids, Thyroid hormones, Vitamin D
Reserpine
Leads to loss of granular storage of norepinephrine
Sedative agents
Produce reduction of anxiety
Selectivity
Comparing the ED50 for different responses to the same drug in vivo
Selegiline
Inhibits metabolism of dopamine
Smooth endoplasmic reticulum
Most CYP450 enzymes located
SSRI
Fluoxetine
Stage 2
Breath holding, retching, irregular respiration
Steady state
First dose / 0.5
Succinylcholine
Shortest duration- depolarization type
Synaptobrevin
Cellular protein promotes fusion of vesicular membrane
Tachyphylaxis
Rapid diminution of a tissues sensitivity to a drug after administration
TCA
Imipramine
TCA excessive quantity
Death
Tetracaine
Ester local anesthetic high potency, long duration of action
Timolol
Reduce MI mortality
TPA
Biotech and cloning genes ex
Transport by diffusion across membranes
Most dependent on the ability of a drug to dissolve in a lipid membrane
Transport proteins
Macromolecule targeted by cardioactive dig glycosides to produce eff on heart
Trazodone
Considerable sedative action , no antimuscatinic side eff
Treatment of alcohol withdrawal
Maintain K and MG balance,
Tubocurarine
Nondepolarizing neuromuscular blocker
Valproate
Absence, complex partial, generalized tonic-clonic, simple partial
Vesamicol
Alters storage of acetylcholine in dense core vesicles
2ndary hypercholesterolemia
Early nephrosis
Abciximab, eptifibatide, tirofiban
Reduces platelet aggregation by bunding to the platelet IIb/IIIa receptor complex
ACE
Altered taste
ADHD
Interference w/ hormone receptors
Alpha receptor of vessels
Nonselective drug action leads to excessive tachycardia
Aminocaproic acid
Inhibitor of fibrinolysis
Amiodarone
Markedly prolong action potential duration
Angiotensin 1
Enzymatic action of renin
Antiatherogenic
HDL
Aspirin
Irreversibly acetylates cyclooxygenase=> inhibition of the synthesis of thromboxane A2
Atherogenic
VLDL, IDL, LDL
Atrial natriuretic peptide
Regulation of Na excretion
B receptors of juxtaglomerular cells
Hypotensive action – propranolol
Blue Monday
Throbbing headaches caused by loss of tolerance
BPH
Avoid K sparing diuretics
Bradykinin
Vasodilator axn-arteries ;contracts veins
Calcium overload
Digoxin induced arrhythmias
Cardiac inotropic actions of digoxin
Consequence of Na/K aTPase inhibition
Ccb+ tachy
Verapamil
CHF = digoxin
Avoid high intake of sodium
Clopidrogel
Blocks adenosine diphosphate receptor on platelets =>reduce platelet aggregation
Colestipol
Inhibits absorption of cholesterol bile acids
Digoxin
Eliminated in the kidney
Dihydropyridine – nimodopine, nifedipine, nicardipine
More selective vasodilator than verapamil (phenylalkylamine)
Diuresis
Elimination of urine volume
ECG induced digoxin
Increasing PR interval
Effect of warfarin
Reversed by vitamin K
Endothelin
Vasoactive peptide – iv injection causes vasodilation followed by vasoconstriction
Furosemide
Altered hearing
Gemfibrozil
Elevated triglyceride levels
Half life of digoxin
Requires 1 week to stabilize pt w/ maintenance dose
Isosorbide dinitrate
Orally effective form of nitrovasodilator
Kidney tubules
African American respond better
Lepirudin
Inactivates fibrin bound thrombin in thrombi
Lidocaine
Shortens the duration of action potential
Low MW heparin
inhibits factor X
Magnesium
Counter the cardiotoxicity of digoxin
Metoprolol
Inhibits catecholamine-induced arr
Niacin
Reduced HDL levels
Nsaids inhibit
Aldosterone antagonists , carbonic anhydrase inhibitor, thiazides, triamterene
NTG
Relaxes smooth muscle
Omega 3 fatty acid ingestion
Lower triglycerides
Organic nitrites
Effective in erectile dysfunction
Pindolol
Partial agonist, ISA
Procainamide
Renal failure, torsade de pointes
Quinidine
Blocks Na channels and increases duration of the action potential
Re-entry phenomena
Abnormalities in cardiac conduction that give rise to abnormal cardiac rhythms
Rifampin
Decrease anticoagulant effect of warfarin by inducing hepatic enzymes that transform the anticoagulant in the body
Simvastatin and lovastatin
Must be converted in GI tract to an active compound
Spironolactone
Hyperkalemia
Streptokinase
Proactivator plasminogen
Sympathetic nerve terminals
Antihypertensive action of reserpine and guanethidine
Unfractionated heparin
Activated partial thromboplastin time
Unstable angina
Decreased platelet aggregation
Vasoactive intestinal peptide
Modulator, relax airway & vascular smooth muscle
Vasomotor center – clonidine
Lower BP
Vasopressin
Increase water absorption
Verapamil
Dependent on Calcium channel blockade
Warfarin
Blocks gamma carboxylation of glutamate residues in factors 2,7,9,10
Iron deficiency
Chronic anemia
Iron dextran
Appropriate for parenteral admin

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