a and l rev
Terms
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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