Flashcards in Drugs Deck (328):
What drug is a first line TB treatment and causes increased nerologic side effects in pts with NAT-2 polymorphism?
What drug causes excessive hypotension along with CYP2D6 polymorphism?
What type of anti-depressants are effected by CYP2D6 metabolism?
poor metabolizers increase side effects
ultrafast metabolizers degrade drug too quickly
What drug is a proton pump inhibitor and is influenced by CYP2C19 polymorphism?
omeprazole aka Prilosec
What drug is an anti-convulsant and is effected by a CYP2C19 polymorphism?
What drug is an anti-platelet and is effected by a CYP2C19 polymorphism?
What drug inhibits platelet aggregation and when you not activated due to polymorphism by CYP2C19 leads to decrease in drug activity and increase in serious CV outcoumes?
What drugs are impacted by CYP2C9 and lead to risk of bleeding/hemorrhage with polymorphisms?
What drug is effected by Vitamin K receptor (VKORC1); and when the clade is different for that VKORC1 leads to different dosing requirements?
CLade A requires low dosing
Clade B requires high dosing
What drug can lead to adverse reactionso f apnea and paralysis when there is a psuedocholinesterase polymorphism?
What drug increases risk for life threatening bone marrow suppression iin patients with decreased thiopurine methyltransferase activity?
P-glycoprotein function in the gut results in increase net uptake of what drug?
cardiac glycoside digoxin
What drug is CYP2D6 poor metabolizer and ultrafast metabolizer has what effect on what drug that can increase side effects or have no benefit?
ultrafast increases morphine side effects
slow causes codeine no benefit
What drugs metabolism is primarily mediated by CYP2C9, acts as a COX1 and COX2 inhibitor as well as an inhibitor of CYP2D6?
What drug helps treat trigeminal neuralgia and is also an anticonvulsant, by acting on Na+ channel to reduce excitability?
What are the drugs that is a tyrosine kinase inhibitor that target the kinase domain of the EGF receptor and inhibit signaling?
What drug is a alpha1, alpha2 and Beta1 agonist
Increases Peripheral Vasc Resistance
Increase mean BP
Therapeutic used for:
vasoconstrictor in acute care
elevate blood pressure
What drug is alpha1,alpha2, beta1, beta2 agonist
increase HR, contractile force, CO
Increase systolic BP, decrease diastolic BP
dose-dependent PVR decrease
Used to treat hypersensitivity rxns
increase duration of local anesthetics
decrease opthalmic hemorrhage
What drug is a Beta1 and Beta2 agonist
Increase HR, Contractile force, mean BP decrease
Emergency Tx of bradycardia or heart block
CardioVasc actions of this drug are dose-dependent
low dose: "renal dose" (D1 agonist) increase renal blood flow
intermediate dose "cardiac dose" increase HR, contactile force, cardiac output (Beta1, D1 agonist)
High dose "pressor dose" vasoconstriction and increased peripheral vasc resistance (D1, alpha1, beta1 agonist)
What drug acts overall as a racemic mixture funtions as a Beta1 agonist?
Increase HR, contractility and CO
Short-term Tx of cardiac decompensation
Cardiac stress test
What is the orally active pro-drug metabolized in nerve terminas and acts as an alpha2 receptor agonist and stimulates central alpha2 to reduce sympathetic outflow.
Major therapeutic use is hypertension
side effects: sedation, dry mouth, edema, rebound hypertension
What is an agonist of alpha1 adrenergic receptor
increase systolic and diastolic blood pressure
reflex decrease in heart rate
decrease blood flow in most vasc beds
opthalmic decrease hemorrhage
admin with local anesthetic
treatment of hypotestant
What is an alpha2 adrenergic receptor agonist
used as an anti-hypertensive by actions in CNS alpha 2 receptors
causes prolonged blood pressure lowering
decreases PVR, HR, CO
dry mouth and sedation, edema, rebound hypertenstion
What is a selective beta2 adrenergic receptor agonist
short acting -3-6 hours
bronchodilator main therapeutic role
tremor , anxiety , tachycardia
What is a beta 2 agonist used by inhalation with a long duration of action 12hrs
used to treat COPD, nocturnal or persistant asthma
slow onset of action, not for acute bronchospasm
What drug is a powerful CNS stimulant in addition to peripheral alpha and Beta receptor actions
effective after oral admin
molecular actions work by releasing NE from adrenergic nerves, weak direct alpha and Beta agonist, competes with NET
used to treat narcolepsy and ADD
Direct agonist alpha and Beta receptors
banned by fda
Direct alpha1, little Beta 2 agonist
less CNS stim
major therapeutic use
Inhibits norepi release and depletes neuronal amine stores
orally active, long acting
don't penetrate into CNS
taken up into adrenergic nerves via NET
Used to treat essential hypertension
orthostatic hypotension, male sexual dysfunciton diarrhea
Guanethidine and Guanadrel
What diffuses into adrenergic neurons and depletes norepi stores by inhibitin VMAT2
orally active, penetrates into CNS
used to treat hypertension
Side effect: sedation, depression, diarrehea, gastric issues
What drug is an irreversible antagonist of alpha1 and alpha2 recetpors orally active, long duration
produces vasodilation proportional to degree of sympathetic tone
treats hypertension with pheochromocytoma
What is a competitive inhibitor of alpha1 and alpha2 receptors
orally active, shorter duration of action 2-4 hours, block can be overcome by increasing level of agonists
hypertension-can only be used in combo with other agents
shorten or reverse DOA of anesthesia
What drug is an orally active, selective competitive anatagonist of alpha1 receptor
little blockade of presynaptic alpha2
decreases vascular tone
produces favorable effect on lipid profile
treats hypertension, short-term Tx of CHF, first dose phenomenom
What drug is an alpha1A antagonist with less blockade of alpha1B atagonist, treats difficulty urinating associated with benign prostatic hyperplasia
What drug is a non-selective Beta antagonist, competitive reversible , has substantial first-pass emtabolism
sedation, impotence, increase airway resistance
What drug is similar to propranolol, therapeutically, non-selective beta adrenergic receptor antagonist, also treats wide-angle glaucoma admin as eye drops
What drug is a 2nd gen beta blocker, Beta1 selective antagonist
competitve, reversible, at low doses is more selective for beta1 receptor
treatment similar to propranolol
treatment of chronic heart failure
What drug si a Beta1 selectie antagonist that is orally active, once per day dosing, doesn't penetrate into CNS, and has similar to propanolol treatment but doesnt do migraine Tx
What 3rd gen beta blocker is a competitive reversiblle antagonist of alpha1 adn both Beta receptors, treats hypertension orally and hypertensive emergencies by IV
What 3rd gen beta blocker is a competitive reversible antagonist of alpha1 and both beta receptors and is sued to treat CHF, hypertension, acute MI
What muscarinc agonist is used opthalmic for rapid miosis?
What quatenary amine, choline ester, has a primary effect on GI/GU system
Used to treat urinary retention in absence of obstruction
What alkaloid is a tertiary amine with predominant muscarinic effect, is used orally for xerostomia and amiotic agent to treat wide angle glaucoma and emergency Tx for narrow angle glaucoma?
What is the non-substrate, competitve acetylcholinesterase inhibitor
rapid onset short duration
doesn't penetrate CNS
Used to treat myastehnia gravis
Distinguish cholinergic from myasthenic crisis
reverse paralysis by competitve neuromusc blcking agents
What alkaloid is reversible aceylcholinesterase inhibitor that acts as a slowly reversible substrate
lipophilic, penetrates CNS
treatment of chronic-wide angle glaucoma
treats toxicity by antimuscariic drug poisoning
What synthetic, slowly reversible, no CNS pen, oral
reversible substrate aceytylcholinesterase inhib is
myasthenia gravis Tx
prevetiono f atony of gut and bladder
reverse of paralysis by neromusc junction blocking
What drugs aare nerve gases, act as irreversible acetylcholinesterase inhibitors?
Sarin, tabun, soman
What is an insectide that can be dangerous as an organophosphate?
What is an insectide that has greater safety as an organophosphate, becasue it is detoxified in higher organisms?
What reactivates Ach peripherally that is used to treat organophosphate toxicity, that must be used quickly in additon to Atropine?
What is a muscarinic receptor antagonist that is used to treat organophosphate toxicity?
Previously used for various GI disorder
Tx of :
mydriasis and cycloplegia
during anesthesia to block vagal reflexes and reduce secretions
What muscarinic receptor antagonist is an alkaloid that has great CNS penetrationa
Motion sickness and vestibular disease?
What semi-synthetic muscarinic receptor antagonist has no CNS penetration and poor systemic absorptionw hen inhaled
reduce bronchial secretions and reduce bronchocontrstion
What synthetic antagonist of Muscarinic receptor has a fast onset (20-40 min) short duration 4-6 hrs
mydriatic and cycloplegic
What synthetic muscarinic antagonist is used to Tx: overactive bladder and incontinence
but has high incidence of anti-muscarinic side-effects:
xerostomia, blurred vision, constipation, drowsiness
What syntehtic antagonist of muscarinic receptor is used to treat overactive bladder and incontincence and has selectiity for M3 subtype resulting in less CNS side effects?
What synthetic antagonist of muscarinic receptor is a quaternary amine and has noCNS pen
parasympathomimetic effects when neostigimine is used to reverse skeletal muscle paralysis by neuromusc blocking agent?
What competitive neuromuscular blocking agents has an intermediate duration, with liver metabolism, minimal cardiovasc effects and no histamine release?
What competitive neromusc blocking agent has an intermiediate duration, spontaneously degrades in plasma, minimal cardio effects and slight histamine
What competitive neuromuscular blocking agent has a long duration of action, eliminated b renal excretion, causes slight increase in HR and BP and slight histamine release?
What drug is a depolarizing neuromuscular blocker, that produces muscle fasciculations and paralysis with an ultra-short duration of action
metabolized by pseudocholinesterase and used frequently to allow tracheal intubation?
What is a competitive antagonist of the leukotriene receptor, used for management and prophylaxis of asthma?
What inhibits the synthesis of of leukotrienes and is used as prophylaxis and chronic tx of asthma.
What drugs act by inhibiting TNF-alpha, acting by binding TNFalpha as a antibody?
What drug is an antiplatelet,NSAID and acts by inihibiting COX 1 adn 2 enzymees via acetylation leading to a decrease in prostaglandin precursor formation?
What drug is used for cervical ripening by break down of collagen and EP4 receptor and termination of early pregnancy by EP1/EP3, increase calcium.
What drug is used to terminate pregnancy by uterine contraction and increase calcium as well as used to tx postpartum hemorrhage after conventional tx?
What durg is used as a replacement therapy for prevention of ulcers caused by long-term admin of NSAIDS by suppression of gastric secretiona nd increase mucosal blood flow?
What is used to treat impotence/erectile dysfuction by intracavernous injection as well as maintenance of patent ductus areteriousus until surgical correction?
What is used to tx primary pulmonary hypertension which is rare, done by continuous IV infusion?
What is used to treat glaucoma by increasing outflow of aqueous humor and EP2/4 receptor as well as used to create eyelash hypotrichosis?
What drug is an endogenous steroid, frequently used as a tx for adrenal insufficiency?
What drug (steroid) has a strong anti-inflammatory potency and causes no sodium retention?
What steroid is more similar to cortisol but with a slightly stronger anti-inflammatory property and slightly less mineral corticoid properties?
What steroid tx has both strong anti-inflammatory potency as well as acts strongly as a mineralcorticoid?
What endogenous steroid has strong mineralcorticoid properties and minimal anti-inflammatory/glucocorticoid properties?
What drugs blocks 11-beta hydroxylation as a syntehsis inhibitor, doesn't inhibit ACTH and is used as a diagnostic test/
What durg acts as a competitive antagonist at progesterone and glucocorticoid receptors. Tx Abortiona nd Cushing disease
What two rugs are competitive at mineralcorticoid receptors. Diureteics that are used to tx hypertensiona nd CHF and hypertrophy?
Sprionolactone and Elperenone
What drug is a progesterone recetpor agonist but a mineralcorticoid antagonist as well as an androgen receptor antagonist. Tx w/ estrogen:: Suppress ovulation and as HRT
What drug is metabolized to 6-mercaptopurine. Inhibits purine biosynthesis. Tx: Inhibit rejection of transplanted organs and in autoimmune diseases
What drug is an alkylating agen that resutls in cross-linking of DNA to kill replicating and non-replicating cells. Toxic effect more suppressed on B cells. Used to tx autoimmune diseases.
What drug is an inhibitor of dihydrofolate reductase, inhibits dna syntehsis and is used to tx autoimmune disease.
Side effect: hepatic diseases
What durg is metabolized to mycophenolic acid. Mechanism of action: lymphocyte selective immunosuppressant. Cannot make GMP via salvage pathway. Inhibit lmphocyte proliferation and expression of cell surface adhesion molcules. Tx: prevent renal allograft and allows lower dose of cyclosporine. Tx rheumatoid arthritis and refactory psoriasis.
What drug is a lipophilic peptide antibiotic. Mechanism of action is it binds to a cellular receptor to preven actionation of IL2 production. Prevents rejection of transplanted organs and used in some autoimmune diseases.
Nephrotoxicity is a major ide effecct--> reversible
What drugs is a FK binding protein that has the same mechanism of action as cyclosporine. 50-100x more portent than cyclosporine with less toxicity.
What durg inhibits t cell activation and proliferation downstream of IL2. Binds FKBP-12. blocks G1 to S transition
What is the chemical name for aspirin?
What drug has a plasma half life of 2 hours, is an anti-inflammatory, anti-pyretic and analgesic that is a COX1 and COX2 inhibitor. Propionic derivative
What drug has anti-inflammatory analgesic and anti-pyretic properties that has a half life of 14 hours. Propionic derived.
What drug is an acetic acid derivative that is a reversible inhibitor of COX 1 and 2. Not routinely used to tx pain and fever.
What drug is a reverisible inhibitor of COX 1 and 2. Absorbed orally and intramuscularly and highly plasma protein bound. Has some advere effects/toxicity.
What is a reversible inhibitor of COX2 preferably but COX1 stillinhibited. Anti-inflammatory analgesic. Pro-drug , has a long half life
What drug is a reversible inhibitor of COX1 and 2. Oxicam derivative. Half life 50 hours. Tx: acute and chronic rheumatoid arthritis
What drug sis a salicylate that functions as an inhibition of IL-1 and TNFalpha, lipoxygenase pathway. No COX inhibition. Used to treat ulcerative colitis, rheumatoid arthritis and AK spondyltiis. Local effect in GI.
What drug is a selective COX2 inhibitor That has a sulfa group. and it used to manage acute pain.
What drug is a para-aminophenol derivative. Mechanism of action is not well understood but is more CNS selective. Only analgeesic and anti-pyretic effects with no anti-inflammatory effects.
What agent inhibits the relase of histamine, is an ant-inflammatory agent. Stabilizes most mast cell membrane and prevents histamine release. Prevents asthma, allergic rhinitis, conjunctivitis and food allergies.
What drug inhibits the release of histamine as a monoclonal antibodies. Can cause hypersensitivity. Subq admin. decreases amnt of antigen specific IgE that normall binds to and sensitize mast cells. Tx allergic asthma.
What are teh two first generation. Ethanolamines. Antihistimine, general anti-histamine effects, with CNS effects
Diphenhydramine (profound drowsiness) and Dimenhydrinate
What first generation anti-histamine is an alkylamine? Less prone to cause drowsiness.
What first generation H1 blockers is also a dopamine2 blcoker. Phenothiazines.
What is a second generation antihistamine that has a higher incidence of sedation than the others? Is derived from piperazines.
What H2 receptor blockers offer relief of symptoms of gastric upset and has a main tx uncomplicated Gastroesophageall reflux? Therefroe have a low incident of side effects. In order of potency from most potent to least.
What H2 receptor blockers is inhibits cytochrome P450, long term at high doses decreases testosterone binding.
What H2 receptor blocker inhibits cytochrome P450 at 10% of the rate of cimitedine?
What are the three second generation of antihistamine drugs.
fexofenadine, loratadine and desloratadine
What is a potent hallucinogen, a full or partial agonist at 5HT2 receptor?
Lysergic Acid Diethylamide
What is a partial agonist at 5HT1A receptors used as an antianxiety agent?
What is an agonist at 5HT1D?
Tx used in migraine headaches
side effects nausea, vomiting, angina, dizziness and flushing
What is an indirect agnoist of serotnin. Blocks reuptake of serotonin into neurons.
Tx affective disorders
What is an indirect agonist of serotonin? Monoamine oxidase inhibitors-- block metabolism of serotonin, NE and DA
Tx of depression and narcolepsy. Food induced HTN
What is a 5HT2 receptor antagonist as well as a H1 histamine antagonist?
Tx of skin allergies, pruritus
What is a 5-HT3 receptor antagonist?
Tx: nausea and vomitting from chemo
GI and brain receptor
What is a selective 5HT3 antagonist used to tx women with predominant IBS
What is a nitrate involved in relaxation of arterial and venous smooth muscle.
Mechanism of action of nitrates is NO donor, intracellular signaling
What drug is involved in relaxation of arterial and venous circulations.
What direct vasodilator, inolved in arterial circulation. Heart failure, hypotension?
Mechanism of action: increases cGMP
Tx hypertension emergencies
Tx severe hypertension
K+ATP channel opener
Fluid retention-use with diuretics
What potassium channel opener is used to treat hypertensive emergencies and hypoglycemia
What calcium channel blocker is pheylalkylamine?
What calcium channel blocker is benzothiazapine?
What are the phosphodiesterase 3 inhibitors. Tx Heart failure through intracellular signaling
Milrinone, Inamrinone, Cilostazol
What are the phosphodiesterase 5 inhibitors, used to tx erectile dysfunction?
What drug is involved in renin-angiotensin blocker. Treats by renin inhibition, lowering arterial and venous circulation?
Angiotensin converting enzyme inhibitor
What drug is a vasodilator, works by dopamine A1 receptor agonists Arteriial and venous circulation.
Involved in renal blood flow and Na secretion
Tx hypertensive crisis
What drug is an alpha-adrenergic blocker. Involved and venous circulation
What bronchodilators are Beta2 agonists?
albuterol, pirbuterol, Terbutaline, salmeterol, formoterol
have some cardiotoxicity
What drug is an anti-cholinergic, works by muscarinic receptor and mucous secretion.
What drug is a bronchodilator, using methylxanthine. Phosphodiesterase inhibition. Adenosinereceptor antagonism
What drug is used to treat hypertension and works as an antagonist of mineralcorticoid? Act as diuretics
spironolactone and eplerenone
What drug is used to treat hypertension and works by blocking AT1 receptor from angiotension 2?
Tx: Improves heart failure
What drugs function by angiotensin converting enzyme inhibitor to inhibit angiotensin 2 formation and bradykinin degradation?
What drug acts as a direct renin inhibitor? Used to treat hypertension; lowers both angiotensin 2 and aldosterone concentration
What is the drug and chemical class of the CCB that is used to treat Angina, Supraventricular arrythmias
Diltiazem (prototype of the benzothiazepine family)
What is the drug and chemical class of the CCB that is used to treat Supraventricular arrythmias?
What is the drug and chemical class of the CCB used to treat hypertension and sometimes angina? Has a fast onset?
What is the drug and chemical class of CCB that us used to treat hypertensions and sometimes angina, has a slow onset and slow affect compared to others in the class?
What drug is filtered in the kidney and acts by inhibiting carbonic anhydrase in proximal tubule; preventing H+ creation for bicarb reabsorption?
Tx: glaucoma, alkalinize urine, anticonvulsant, altitude sickness
Acetazolamide (carbonic anhydrase inhibitor)
What diuretic function by increasing osmolality in the tubular lumen. Relaively weak diuretic?
What drug is filtered and secreted by OAT, and inhibits Na-K-2Cl symporter? Increase excretion of Na, K, Cl and H20.
Tx: Edema of Cardiac, hepatic or renal origin
Acute pulmonary edema
Bumetanide, Ethacrynic Acid, furosemide (Loop diuretic)
What loop diuretic has the unique side effect of hyperglycemia?
What mechanism work by inhibiting Na/Cl symporter anda ct on cortical segment of distal tubule. Increase secrion of Na, K, Cl, H20. Long duration of action and moderate onset.
Tx: Edema due to CHF
Hypercalciuria (Ca salt-renal)
What drug block action of aldosterone on collecting duct?
Tx: Edema, HTN, Improved survival in heart failure
What drug is a potassium sparing diuretic that acts by blocking sodium entry into principal cells of collecting duct?
What drugs act by dilating hte renal vasculature, increases RBF wihtout changing GFR.
Dopamine, Fenoldapam, Caffeien Atriopeptins (renal vasodilators)
What drug is highly negative charged and works by binding Antithrombin and catalyzing the inhibition of several coagulation factors. It is a suicide inhbitor for these proteases?
Tx: venous thromboemoblism, Cardiopulmonary bypass, prophylatic use to prevent venous thrombosis
What drug works by catalyzing the inhbiition of factor Xa only by antithrombin?
Low molecular weight heparin
Tx: venous thromboemoblism
prophylaxis of venous thrombosis
What is an IV admin drug that is 65 AA and binds tightly to both catalytic sites of thrombin?
Tx alternative to heparin in coronary angioplasy or cardiopulmonary bypass surgery
What drug is synthetic, 20 AA polypeptide and occupies the catalytic site of thrombin. Thrombin slowly cleaves it.
Tx as an alternative to heparin in coronary angioplasty or cardiopulmonary bypass surgery.
What drug is an IV administered direct factor Xa inhibitor? Tx: prophylaxis of DVT in pt undergoing surgery; tx of acute PE and DVT.
Prophylaxis with a history of HIT
What drug is an orally administered prodrug, that directly inhibits thrombin both free and fibrin bound. Shouldn't be admin with Pgp inducers.
What drug is an oral direct-acting facotr Xa inhibitor. Binds reversibly to factor Xa. Tx: reudicng risk of stroke and embolism with A fib pts. Prophylaxis of DVT?
What endogenous activator works by bnding sites on fibrin that are inclose proximity to plasminogen binding site. It activates fibrin-bound plasmin to initate clot resolution.
tissue-type plasminogen activator (t-PA)
What drug is a t-PA and is used to tx: ST-elevation in MI (STEMI)
management of acute ischemic stroke
management of acute pulmonary embolism?
What drug is a synthetic lysine analog. That blocks the states associated with an excessive breakdown of fibrin.
Tx: hemorrhage with surgical procedures, replace factor 9, anti-hemophilic factor, desmopressin
What drug is an anti-platelet drug that works by phosphodiesterase inhibition/and or blockade of adenosine? Tx prevention of thromboemoli with wafarin?
What drugs inhibit ADP biding to P2Y12 receptor. They are irreversible antagonists that inhibit platelet for it's lifetime?
Clopidogrel, Prasugrel, Ticlopidine
What drug inhibit ADP biding to P2Y12 receptor. Similar to clopidogrel but reversible properties?
What drug is an Fab fragment of a chimeric human-murine monoclonal antibody. Prvents platelet aggregatio by binding GP IIa/IIIa. Tx prevent thrombosis in pts undergoing coronary angioplasty and stent placement. prevent vessel restenosis, reinfacation,
What drug is primarily used to in persons with unstable angina and MI often in combination with LMWH; prevent thrombosis in unstable angina or non-ST-segment elevation?
What drug given by IV or subq by interaction with anti thrombin? Can be countered with protamine sulfate and interacts with factor ten and not thrombin?
Enoxaparin and dalteparin
What drug is used to induce anesthesia; has a long half life, barbituate
intra-arterial injection can produce severe inflammation and be necrotic
side effects CV produce vasodilation
CNS reduce cerebral oxygen
What drug has an onset and duration of anesthesia as the same as barbituate
used to induce and maintain anesthesia
causes pain on injection otherwise similar side effect profile to barbituates
What drug is used to primarily used to induce anesthesia in patients risk for hypotension
high incidence of pain on injection and myoclonus
side effect profile similar to thiopental but less CV resp profile
more nausea and post-surgical mortaility due to adrenocortical stress response
what drugs is a dissociative anesthesia; characterized by profound analgesia, unresponsive to commands, amnesia, spontaneous respiration
side effects increase ICP produce nystagmus, emergence delirium, increase BP
used mainly in children and pts with bronchospasm
What drug is a short acting benzo used for concious sedation, induction agent, ajunct; anti-anxiety
slower induction time than thiopental
metabolized by hydroxylation
caution in parkinson's and bipolar
What gas anesthetic
excreted unchanged from lung
induce and maintain anesthesia
co-admin of nitrous oxide
What anesthetic is very volatiles and needs special equipment to admin
tx outpatient surgery, coughing and bronchospasm
direct skeletal muscle relaxation
similar to isoflurane
What drug has a very low blood gas partiition coefficient
5% admin is metabolized to fluoride ion in liver
tx inpatient and outpatient maintenaince
not a respiratory irritant
What anesthetic is a true gas
very insoluble in blood
rapid uptake from alveolae results in conc of gases
dilute oxygen when use discontinued
produce sedation and analgesia
adjunct with other inhalational anesthetic
resp effects are minimal
What local anesthetic
blocks norepi uptake
tx topical anesthetic for upper respiratory tract where its actions as both a vasoconstrictor and local anesthetic provide anesthesia and shrinking of mucosa limit bleeding
What local anesthetic is a short acting ester local anesthetic
first synthetic local anesthetic
has been supplanted by newer agents but still used for infiltration anesthesia
low potency, slow onset, and short duration of action
What local anesthetic is a long acting ester local anesthetic
more potent and longer duration of action
widely used in spinal anesthesia and in topical and opthalmic preparation (not irritating when in eye)
rarely used for nerve block
What local anesthetic has low solubility in water, therefore too slowly absorbed when applied topically
applied to wounds and ulcerated surfaces for long period relief
what amide local anesthetic
produce faster more intense long lasting than an equal conc of procaine
used with epinephrine decreases rate of absorption
metabolized in liver
wide range of use
What long acting amide local anesthetic capable producing prolonged anesthesia
long duration of action plus its tendency to provide more sensory than motor block
dissociates from Na+ channesl slowly resulting in increased potency
What is a long acting amide local anesthetic consists of S-enantiomer
similar to bupivicaine with less cardiotoxicity
epidural and regional anesthesia
more motor sparing
What is the most common anti-depressant
common side effects; nausea, insomnia, nervousness, sexual dysfunction
acute toxicity is low
clinical use for Major depressive, OCD, Panic disorder, social phobia, PSTD, GAD, PMS
this one has long-half life
What drug is an SSRI that has a shorter half life than fluoxetine
What drug blcok serotonin and norepi uptake; 12-18 hour half life.
Caution in pts with liver disease
tx fibromyalgia, diabetic neuropathy, back pain and osteoarthritis in addition to SSRIs
What drug is an atypical antidepressant; approved for nicotine withdrawal and SAD
blocks norepi and dopamine uptake
What drug blocks presynaptic alpha2 receptors in brain and increases appetite
What drugs is a tricyclic antidepressant; rapidly absorbed and has a long plasma half life
produces elevation of mood
prominent anticholinergic effects
TX Major Depression
enuresis in childhood
What tricyclic antidepressant treats obsessive compulsive disorder?
What typical antipsychotic has low to medium potency, sedative, pronounced anticholinertgic actionsl aliphatic side chains?
What piperidine side chain typical antipsychotic
less extrapyramidal actions
What piperazine side chain typical antispychotic with high potency, less sedative, less aticholinergic more extrapyramidal reactions?
What butyrophenone derivative is not chemiclaly related to phenothiazines but is similar to the high potency piperazine derivatives?
What atypical antipsychotic has less extrapyramidal side effects that may cause seriosu agranulocytosis or other blood dycrasias ina small percentagge of patients
effects negative symptoms
What drug is related to clozapine but a more potent 5-HT2 antagonist; few extra pyramidal symptoms
What combined dopamine and serotonin receptor antagonist has a low incidence of extrapyramidal side effects.
What structurally related to clozapine with effects on D2 and 5-HT2 receptors; abuse potential
What d2 partial agonist approved as an adjunct in tx of depression
What drug si a monovalent cationl blocks manic behavior by blocking the IP2 recycling to pIP2
narrow therapeutic window
What drug acts as a maintsaty for antiseizure therapy, bipolar 1 disorder, acute manic/mixed episodes
mechanism of action blcoks sodium channels
What drugs are carboxylic acid with anti-seizure activity
blocks repetitive neuronal firing
may reduce T-type Ca2+ currents
increase GABA conc
valproic acid and divalproex
What benzodiazepine primarily used for hypnotic actions?
What benzodiazepine has a rapid absorption orally and used as a muscle relaxant?
What imidazopyridine derivattive binds benzodiazepine receptor but is less disruption of sleep architecture and has a lack of muscle relaxant effects
What barbituate is used as a hypnotic?
What aldehyde hydrate is used as a sedative hypnotic; less effects on stages of sleep than benzo and barbiturate
What drug is a GABA mimetic agent that works at GABAB recptors
results in hyperpolarization causing presynaptic inhibiton
tx muscle spasticity
What drug is an alpha2 adrenergic anist that is related to clonidine
may have similar efficacy to diazepine in relieving muscle spasm
What drug inhibits acetaldehyde metabolism by inhibitin aldehyde dehydrogenase?
What benzodiazepines are used to treate alcohol withdrawal syndrome to prevent seizures, agitation and mood swings?
diazepam and chlordiazepozide
What drug is used to reduce urge to drink by acting as opioid receptor antagonist
best with psychosocial therapy
What drug decreases drinking frequency and reduces relapse by actingas a GABA mimetic
side effect diarrhea
What drug is a methylxanthine compound that blocks adenosine receptors
blocks inhibitory efffects of adenosine
What drug si a psychoactive alkaloid; weak base
metabolized by serum and liver esterases
ptent inhibitor of reuptake of norepi dopamine and serotonin
What drug is alpha-methyl phenethylamine derivative
well absorbed orally
long duration of action 4-6 hours
deaminated to benzoic acid as well as excreted unchanged
relases norepi, dopamine, and serotonin
amphetamines and amphetmine like drugs
What drug is structurally and mechanistically similar to amphetamines and used to treat ADHD
What drug is an agonist of nicotinic cholinergic receptor
affects mainly autonomic ganglia sympathetic ganglia activation results in release of epinephrine and parasympathetic ganglia activation is predominant results in nausea
CNS receptor activation resls in membrane excitation
What drug has an unknown mechanism of action seems to enhance noradrenergic and dopaminergic signaling
moderatively effective reduces craving and nicotine withdrawal symptoms
What drug is a partial agonist of CNS nicotinic receptors
reduces craving and withdrawal and reduces effects of full agonist
danger increase suicide depression
What drug is a mu agonist;
low oral to parental potency ratio
duration 4-5 hours
What drug is more lipophilic than morphine
converts to 6-mono-acetyl morphine and morphine
What drugs are used for mild to moderate pain
some is metabolized to morphine
cannot reach same efficacy as morphine
What antibiotic is used to treat gram-pos anaerobes
and 1st line treatment for syphillis
good activity against anthrax, Listeria, Actinomyces
Which one is more acid-stable?
penicillin G and V
V is more acid stable
What drugs are used for Beta-lactamase producing staphylococci, still penicillins?
methicillin and oxacillin
What beta-lactam is used to treat beta-lactamase negative gram positive and gram negative
alternative choice for Lyme disease
ampicillin and amoxicillin
What beta-lactam is a broad gram-negative including
Pseudomonas aeruginosa, Enterobacter, some anaerobes
What beta-lactam is used to treat broad gram negative spectrum inclduing some pseudomonas and Klebsiella including those ticarcillin resistant
What are the two beta-lactamase inhibitors and how do they function?
clavulanic acid and tazobactam
What are the two drugs in the first generation of cephalosporins?
cefazolin and cephalexin
What are the two drugs in the second generation of cephalosporins?
cefuroxime and cefoxitin
What drug is a fourth generation cephalosporin
What drugs are third generation cephalosporin?
ceftriaxone and ceftazidime
What first generation cephalosporin is best gram positive activity of the cephalosporins?
What first generation of the cephalosporins is taken orally?
What is hte only second generation of cephalosporins to penetrate CSF?
What is the only second generation cephalosporin also good for anaerrobes including bacteroides?
What is the third generation cephalosporin that is the therapy of choice for gonorrhea and an empiric therapy for meningitis?
What is the third generationof cephalosporin that is effective against many strains of Ps. aeruginosa?
What is the cephalosporin taken by IV, 2 hour half life, spectrum similar to ceftazidime except more resistant to type I Beta-lactamases. Empirical tx of serious inpt infection.
What is Beta lactam that is admin by IV. Well distributed broad spectrum, several gram pos aerobes and anaerobes. Resistant to many Beta-lactamases including ESBLs?
Tx mixed or ill-defined infection; those not responsive or resistant to other drugs.
What is used against gram-negative aerobic rod. Not useful against gram positives and anaerobes. Resistant to many Beta-lactamases. Can be used in those with known hypersensitivies to penicillins.
What is a glycopeptide antibiotic. Bacteriacidal. Inhibits cell wall syntehsis by binding to free carboxyl end (d-Ala-D-ala)?
Tx gram pos only including MRSA
What antibiotic inhibits synthesis of peptidoglycan building blocks by inactivaating enlopyruvyl transferase, an early stage cell wall syntehsis enzyme?
Tx uncomplicated UTIs caused by E. Coli
What is the polypeptide, not a Beta-lactam. Interferes with cell wall synthesis by interfereing with lipid carrier that exports early cell wall components through cell membrane.
Tx topical use only
What drug is used topically esp for Psuedomonas.
Rare IM or intrathecal use for serious Gram negative infections.
What antibiotic binds to bacterial cytoplasmic membrane causing rapid membrane depolarization.
Tx MSSA, MRSA, strep, enterococcus
NOT FOR PNEUMONIA
What are the two fluroinated quinolones used to trx UTI mainly enterobacteriaceae and uncomplicated gonorrhea?
What fluroinate quinolone tx infectious diarrhea, skin infections, respoiratory infections and bone and joint infections?
What antibiotic has better gram positive activity than many quinolones, targets respiratory infxns except for strep throat, community acquired pneuomnia, and bacterial bronchitis.
Is a quinolone
What drug works by having nitroreductase converting them to reactive compounds which can damage DNA?
What inhibits RNA syntehsis by binding RNA polymerase Beta. Bacteriacidal
Primarily tx pulmonary TB
prophylaxis of H. influenzae type B
and meningococcal meningitis
What is noncompetitive inhibitor of RNA polymerase, thereby inhibitin RNA syntehsis. bacteriacidal.
Tx C dif as a third line
poorly absorbed when taken orally
What tx anaerobes by reduce the nitro group and resulting in DNA disruption.
Tx C. diff (mild/moderate)
combo tx for H. pylori
What are the two aminoglycodsides used to tx Psuedomonas aeruginosa, Klebsiella, Enterobacter, serratia, and more efffective against gram neg than pos?
What is the aminoglycoside used when bacteria show resistance to gentamicin adn tobramycin?
What are the two modern drugs taht are transported into cells by a protein-carrier, bind to 30S subunit prevent attachment of aminoacyl-tRNA to acceptor site. Bacteriostatic
minocycline and doxycycline
What drug is a bacteriostatic, binds 30S ribosomal subunit and blocks aminoacyl-tRNA entry and binds additional unique sites in ribosome.
Tx skin/skin structure, complicated intraabdominal infections, and community acquired pneumonia?
What drugs interferes with binding of aminoacl-tRNA to 50S subunit and inhibits peptide bond formation. Tx broad spectrum; but very serious side effects.
tx brain abcesses and alt tx for meningits
What macrolide is primarily used against gram positive and atypical bacteria; inhibits CYP3A4 metabolism and increase CV problems?
What macrolide is used as an alt to erythromycin for tx of resp infections and has an expanded spectrum to include penicllin resistant Strep, H. pylori, H. influenzae, Moraxella?
What drug is usd to tx resp infections, better gram negative activity tha other macroliedes adn tx chlamydia, neisseria ghonorrea with fewer adverse effects?
What drug has a macrolide like mechanism and inhibits most gram positive cocci and many anaerobes. Not for nosocomial MRSA, enterococcus or gram neg aerobes. Serious colitis?
What drug is used to treat VRE, MRSA, Strep A and B, Strep Pneumoniae but is ineffective against anaerobes and gram negatives. INterferes b binding 50S ribisomal subnit interfrese with 70S formation?
What sulfur based drug is used topically for burn patients?
What drug is most often given with trimethoprim in order to treat UTI, bacillary dysentery, and typhoid fever
What drug works by inhibitin folate syntehsis in bacteria by competitively inhibiting dihydrofolate reductase?
Trimethoprim often used in combo sulfamethoxazole
What are the first line drugs for TB therapy?
What antibiotic is a cidal for activley growin bacilli inhibits synteshis of mycolic acid activated by catalase peroxidase (KatG protein) and targets the enoyl-acyl carrier protein reductase?
What first line TB drugs, inhibits DNA-dependent RNA pol, thereby suppressing RNA synteshis is effective in combo and never used alone. Used for other antibacterial drugs? Use d in combo with Isoniazid most often?
What TB drug interferes with arabinosyl transferase, blocking cell wall synthesis; is a tuberculostatic but doesn't interfere with cidal effects. Is not hepatotoxic and has optic neuritis (5-15%)?
What TB drug is particulary important block mycolic acid synthesis by inhibiting fatty acid synthase I? Important in shot term ttx and useful for CNS involvement. Has sever hepatotoxicity?
Adverse severe potentially fatal hepatitic damage esp when combined with rifampin
What aminoglycoside is used to Tx TB binds to several ribosomal sites causes mRNA misreading and stops initaition by binding at 30S/50S. Least used of first line TB and reserved for most serious forms of TB.
Adverse ototoxicity and nephrotoxicity
What drug is a single-agent prophylaxis of M. avium-intracellulare (MAC) in AIDS pts? Is a lipophilic rifampin analog. Similar adverse effects to rifampin but less frequent
What drug is a part of multi-drug regimen for tx of M. avium-intracellulare in AIDS. Also for MAC prophylaxis. cidal
What drug is used to tx Hansens disease is a structural analog of para-aminobenzoic acid (PABA) inhibits synthesis of folic acid.
prophylaxis of Pneumocystis jiroveci
adverse hemolytic anemia and methemoglobinemia
What drug is used to treat leprosy. Binds to DNA, interfering with reproduction and growth. Used only in combination Adverse effects well tolerated, red-brown pigmentation.
What drug is the gold standards to treat systemic fungal infections? Total cumulative dose is important for renal toxicity. Side effects: hypotension, hypokalemia, tachypnea, 90% show nonpermanent nephrotoxicity.
What anti-fingal is used to treat serious infections, Candida, cryptococcus. Septicemia, endocarditis, meningitis, urianry and pulmonary infections. Used in conjunction with amphotericin. Inhibits thymidylate synthetase and thus DNA syntehsis activated by fungal cytosine deaminase?
What are the two classes of azoles used for serious fungal infections?
Imidazoles and Triazoles
What triazole is used to treat cryptococcus, meningitis, Candida many sites including CNS and urinary sites. Spectrum some albicans and glabrata not krusei? Mainly treatment of superifical Candida infections.
What triazole is used to treat blastomyces, histoplasma, Canddia only esophogause and oropharynx. Candida spectrum is more albican and glabrata. Some krusei unlabelled?
What triazole is used to treat Aspergillus. Fusariu, scedosporium candida (not urinary) tx candida glabrata and krusei?
What drug is used for the treatment of invasive Aspergillus. Candida, esophageal and systemic. Mechanism inhbiits fungal cell wall synthesis by noncompetitively blocking syntehsis of Beta(1,3)-D-glucan in filamentous fungi. results in cell lysis
well tolerated, fever, flushing, phlebitis
What drug is used to treat superficial myoces in an opthalmic infection? Mechanism to amphotericin B.
What drug is used to topically for candida, oral troches or vaginal creams/solutions. Side effect for oral troche include abnormal liver function.
What drug as a mechanism similar to amphotericin B and is used topically for candida at skin, mucous membranes, vaginal infection, GI tract. Topically well tolerated. Can be taken orally for GI candida infections.
What are teh topical treatment for dermatophytes that are azoles?
What few toxic reactions, likely inhibits fungal ergosterol synthesis are (cream/spray/powder)?
What treatment for dermatophytes are inhibiting metal-dependent fungal enzymes by metal-chelation; only FDA-approved topical rx for mild to moderate fungal nail infections.
What oral treatment for dermatophyte, used in a 12-week therapy for nail infections that remain in skin after therapy stopped? Prevents ergosterol synthesis, squalene accumulates, forming lipid droplets that disrupts fungal cell membrane.
What drug is used for recalcitrant dermatophytic infections of skin. Therapy for children esp for tinea capitits. Long term treatment..Mechanism slowly deposited in skin, interferes with microtubule function/mitotic spindle/ mitosis; arrests fungi in metaphase of mitosis
incorporated into keratin precursor cells
Side effects: contraindicated in those with porphyria and advance liver disease; increased metabolism; caution in those with penicillin allergies
What is used for Influenza A prophylaxis and treatment. Blocks viral uncoating by interfering with influenza A m2 protein. Side effects include CNS effects?
What is used to treat influenza A and B treatment/prophylaxis. The drug is a prodrug converted by hepatic esterases. Competitively inhibits influenza neuraminidases; interferes with viral release and viral penetration. Side effects of bronchitis and nasuea>
What drug is an antiviral drug; thymidine analog, interferes with DNA synthesis. Opthalmic useonly used for treatment of kerato-conjunctivits, keratitis and herpes simplex 1 and 2.
what drug is phosphorylated 40-100 times faster in infected cells; inhibit herpes DNA pol 10-30 times effectivively than host cell. Competes with deoxy-GTP for DNA pol.
can be used both orally and IV
What prodrug is complex with multiple intermediates the activie form is penciclovir-triP. Used to treat acute herpes zoster and recurrent genital herpes.
What drug has a mechanism similar to acyclovir. and sed to tx recurrent herpes of lips and face.
what drug is used as a guanosine analog that must be phosphorylated to become active; and is activated by mono-phos by CMV protein kinase? Tx CMV retinitis and prophylaxis in transplant.
What drugs inhibit CMV DNA pol by binding to pyrophosphate binding site. Doesn't require conversion to triphosphate form to be active. Tx CMV retinitis and acyclovir resistant herpes. Side effects: renal damage, electrolyte imbalance, seizure.
What drug is approved for hepatitis B and HIV. Is a nucleoside analog, inhibits reverse transcriptase domain of the hepatitis B. Well tolerated; nausea?
What is the adenosine monophosphate analog; inhibits the reverse transcriptase domain of the hep B DNA polymerase. Approved for hepatitis B Side effect GI upset
What interferes with viral mRNA synthesis by mono-P form inhibits IMP and thus GMP synthesis. Tri-P form inhibits GTP-dependent capping of viral mRNA? Tx infants and young children wiht severe RSV infection. Oral for hep C?
What is reversible inhibitor or NS3 protease of hepatitis C, blocks formation of infectious virus. Tx approved for hep C.
Side effects of anemia, neutropenia, contraindicated with CYP3A substrates or inducers
What is thymidine nucleoside analog, phosphorylated by cellular kinase, Inhibits RT and acts as a chain terminator?
Zidovudine or AZT
What drug inhibits RT by competing for incorporation into DNA causing chain termination, nucleotide prodrug. Tx HIV in combo; well tolerated
What is a nucleoside analog inhbitor of reverse transcriptase. Synergistic with AZT against HIV. Strains more resistant are more susceptible to AZT
What drug is fluronated analog of lamivudine; same mechanism and resistance as 3TC and has some activity against Hep B?
What drug is anucleosdie analog inhibitor of Reverse transcriptase phosphorylated by cell enzymes to active drug. Adverse effect associated with hypersensitivity
What drug is a non-nucleoside inhibitor of reverse transcriptase, binds at different site than NRTIs, disrupts active site of RT. Well tolerated but CNS/psychiatric symptoms.
What drug is a protease inhbiitor but is rarely used for this mechanism and is instead used to block metaboilsm of other protease inhbitirors?
What drug is aprotease inhibitor and therefroe prevents viral aspartic protease from cleaving Gag-pol polypeptide into sepearte functional proteins. Competitive inhibiotr of protease active site. Toxicitiy diabetes, alteration i lipid metabolism, fat redistribution.
What drug is used against HIV-1 only and normally used for tx-experienced pts who failed mulitple regiments. Binds gp41 subunit of HIV glycoprotein blocks conformational changes required for fusion to CD4 cells?
What drug is a CCR5 antagoist and used for tx of HIV-1 tropic to CCR5.
Hepatotoxic and CV evens
What drug is used to treat HIV-1 by working as an integrase inhibitor. Inhibits integration of HIV DNA into genome. Well tolerated some hypersensitivity.
What drug is used to treat many intestinal roundworms and kills some ova. Poorly absorbed from GI tract?
What drug is used to treat hydatid cyst disease and cutaneous larval migrans. Well distributed. Mechanism immobilizes and kills parasite by selective damage to microtubules?
What anti-parasite inhibits energy metabolism of hook worm and blocks microtuble assembly of strongyloides. Tx cutaneous larva migrans.
What drug works as a depolarizing neuromuscular blocker in parasites; poorly absorbed from GI tract. Effective for hookworm, pinworm and roundowrm.
What anti-parasite increases calcium permeability and is drug of choice for Schistosoma? also for Taenia solium bc kills eggs and avoids cysticercosis
What drug treats neurocysticercosis and is agent of choice?
What anti-malarial is concentrated by parasitized erythrocyte by pH dependent mechanism and inhibits heme polymerization allowing it to become toxic to malaria.
Tx prophylaxis for all sensitive 4 species of malaria.
Doesn't clear P. vivax or ovale bc in liver
What drug is similar to chloroquine and is used to treat chloroquine resistant falciparuma nd viviax. Contraindicated in those with epilepsy?
What drug blocks pyrimidine synthesis? Is an antimalarial
part of combo one selectively inhibits mitochondrial electron transport and one inhbiits malarial dihydrofolate reductase.
Atovaquone and Proguanil
What anti-malarial is also an antibiotic syntehsis works by decreasing malarial protein synthesis and depresses dihydroorotate dehydrogenase. Tx of multi0drug resistant P. falciparum
What drug is used to kill liver hypnozoites; radical cure/terminal prophylaxis of P. vivaz and P. ovale. Also used in treatment of Pneumocysitis jiroveci pneumonia in AIDS pts in combo with clindamycin. 2nd line therapy
What drug is used for tissue amebicidie and systemi infection of E. histolytica?
What is a luminal amebicide; with serious side effects associated with high dose or prologned tx. Contraindicated in thsoe with hypersensitivity to iodine
What drug is a luminal amebicide, aminoglycoside tat inhibits protein synthesis. Oral dose very poorly absorbed/
What drug is the drug of choice of Giardia and trichomonas vaginalis?
What drug is used to treat cryptosporidium parvum and giardia lamblia. Inhibits pyruvate: ferredoxin oxidorecutase