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α2 agonist
β antagonist
α1 antagonist
AChE inhibitor, carbamate type
β2 agonist
5-HT1 Receptor
-G-protein coupled serotinin receptor
-Hyperpolarizes cell by increasing K+ conductance
-High concentration in the basal ganglia
5-HT2 Receptor
-G-protein coupled serotonin receptor
-Lead to slow depolarization of the cell by decreasing K+ conductance
-Located in the prefrontal cortex
5-HT3 Receptor
-Ligand gated serotonin receptor
-Rapid depolarization of the cell by increasing Na+ conductance
-Located in parasympathetic terminals in the GI tract and in CNS regions involved in the emetic response

-Inhibition reduces nausea
-Metabolism inhibited by Allopurinol
-Thiopurine-S-methyltransferase deficiency slows metabolism; leads to increased risk of hematopoietic toxicity
α1 receptor
smooth muscle contraction
α2 receptor
-CNS decrease sympathetic system
-Presynaptic decrease release
β1 receptor
-Sympathetic response
-Heart - increase rate, contractility
-Kidney - increase renin release
β2 receptor
-Sympathetic response
-Smooth muscle relax

Disease Modifying Antirheumatic Drug

-Selective costimulation modulator; inhibits T-cell activation
-Used to treat adult rheumatoid arthritis and juvenile idiopathic arthritis

Anti-Platelet Agent - Glycoprotein IIb/IIIa Antagonist (GPI)

-Fab fragment of monoclonal antibody
-One of most effective anti-platelet agents

-Prevents platelet aggregation by binding to the platelet glycoprotein IIb/IIIa receptor and preventing the binding of adhesive glycoproteins (fibrinogen and vWF)

-Acts at final common pathway of platelet aggregation

-Administered IV; long half life
-Primary benefit seen in high risk patients

-Adverse Effects: bleeding; thrombocytopenia; anaphylaxis on reinjection
-Restores normal NMDA signal tone
-Reduces cravings for alcohol
-Reduces withdrawal symptoms due to overstimulation of glutamate receptors
ACE Inhibitors
-Inhibit conversion of Angiotension I to Angiotensin II
-Decreases breakdown of the vasodilator bradykinin (causes cough)
-Decreased hypertensive response to Angiotensin I, but not to injection of Angiotensin II

-May decrease GFR in bilateral renal artery stenosis
-May decrease albuminuria and stabilize renal function in chronic renal disease
-Decreases symptoms and increases survival in CHF

-Adverse Effects: cough, angioedema, hyperkalemia (esp. with NSAIDs, β-blockers, renal insufficiency)

(Paracetamol, Tempra, Tylenol)
-Analgesic and antipyretic
-Weak anti-inflammatory agent

-Overdose (>4g/day) can lead to fatal hepatic necrosis
-Chronic alcoholism increases risk of hepatic necrosis
Carbonic Anhydrase Inhibitor

-Decreases NaHCO3 reabsorption
-Used for treatment of glaucoma

-Adverse Effect: metabolic acidosis
Cholinergic neurotransmitter

-Very short half-life due to rapid hydrolysis
-Formed from ACoA and choline via choline acetyltransferase enzyme

Disease Modifying Antirheumatic Drug

-Binds specifically to TNFα to block interaction with p55 and p75 TNF receptors
-Increased risk of tuberculosis, invasive funcal infections, and other opportunistic infections

Antiarrhythmic Agent

-Used for conversion of paroxysmal supraventricular tachycardia

-Binds Adenosine-R - Slows AV conduction; increases refractory period at AV node

-Very short half life - IV administration

-Adverse Effects: facial flush; headache; hypotension; arrhythmias; heart block; asystoly (transient or prolonged); dyspnea

-Drug interactions with: methylxanthines (caffeine) which block receptor; dipyridamole blocks uptake enhancing effect

(Proventil, Ventolin)
Short Acting Selective β2 agonist

-For bronchospasms, asthma, COPD
-Relax airway smooth muscle and inhibit function of inflammatory cells
-Therapy of choice for relief of acute symptoms and prevention of exercise induced bronchoconstriction

-Adverse Effects: Dose dependent sympathomimetic type effects
Renin Inhibitor

-Decreased plasma renin activity, decreased angiotensin I and II levels
-Increased plasma renin concentration

-Adverse Effects: diarrhea, angioedema, cough, hyperkalemia
Inhibits xanthine oxidase - decreases uric acid production

-Used for gouty nephropathy, chronic tophaceous gout, renal urate stones, secondary hyperuricemia
-Metabolite oxypurinol is also potent xanthine oxidase inhibitor

-6-mercaptopurinol metabolized slower, so dose must be lowered


-Recombinant tPA
-Requires fibrin for activity, so only active at site of clot (unlike streptokinase)
-May also be able to lyse more heavily cross-linked fibrin

-Used to treat MI and acute ischemic stroke

-Adverse Effects: bleeding (intracranial hemorrhage); arrhythmias
-Increases synaptic concentration of dopamine
-Frequently used with levodopa to treat Parkinson's disease
Sodium Channel Blocker (K-Sparing Diuretic)
Aminocaproic Acid

Hemostatic Agent

-Binds reversibly to plasminogen and blocks binding to fibrin and activation of plasminogen to plasmin

-Used to enhance hemostasis when fibrinolysis contributes to bleeding
-Not approved for use in bleeding associated with fibrinolytics
-Contraindicated in DIC
Class III Antiarrhythmic

-Used for serious ventricular arrhythmias; some supraventricular arrhythmias
-Increases refractory period by increasing AP duration - blocks K channels, lengthens QT interval
-Blocks Na channels
-Blocks Ca channels
-Eliminated by liver with long half life - Inhibits some CYP

-Adverse Effects:
-Decreased HR, AV block
-Pulmonary fibrosis, potentially fatal
-Hyper- or Hypo- thyroidism because drug contains I atoms
-Corneal microdeposits seen in all treated for a few weeks (could decrease visual acuity)
-photosensitivity; blue-grey skin discoloration
-Increased ALT, AST
-Peripheral neuropathy
-Can worsen arrhythmias; torsades de pointes uncommon though
-Decreases elimination of warfarin, digoxin

-Short to intermediate acting (3-6 hours)
-Older drug, formerly used as a sleep aid

Second/Third Generation Antidepressant

-Metabolite of antipsychotic loxapine
-Retains some antipsychotic activity
-DA receptor antagonist, may have extrapyramidal side effects

Indirect adrenergic agonist

-Stimulates release of catecholamine from monoamine terminal
-Major CNS action, elevation of central DA levels -> positive reinforcement
-(treatment of ADHD)
-(schedule II DEA-controlled agent)


-Little analgesic activity
-Causes respiratory depression
-Potent Dopanine agonist

-Used to induce vomiting, acting on the CTZ
-Used for temporary relief or as a rescue drug from off-periods of akinesia in Parkinson's disease
-Major side effect: nausea
Cholinergic alkaloid

-From Betel nut (chewed in Orient)
-Muscarinic ~ Nicotinic

-Used in patients with HIT
-Directly inhibits thrombin, including clot-bound thrombin
-Reversible inhibitor

-Short half life with hepatic metabolism

-Can increase INR complicating warfarin transition
-No antidote

Atypical Antipsychotic

-Adjunct therapy in depression and bipolar disorder
Local Anesthetic

-Newest local anesthetic
-High ability to penetrate barriers allows it to be used to penetrate thick bone
NSAID; Weak Anti-platelet Agent

-Analgesic, antipyretic, anti-inflammatory; other uses: juvenile rheumatoid arthritis, decreased incidence of MI, decreased incidence of colon cancer
-Inhibits prostaglandin synthesis by irreversible acetylation of cyclooxygenase
-Anti-aggregatory effects on platelets last lifetime of platelet

-Side effects: tinnitus or deafness, transient decreased renal function, GI intolerance, hepatotoxicity, hypersensitivity
-Contraindications: ulcers, asthma, gout, Reye's syndrome

β1 receptor antagonist

-Cardioselective, β1 >>> β2
-Treatment of htn, angina

-Adverse Effects: Decreased contractility may worsen heart failure, bradyarrhythmias, prolonged hypoglycemia, increased triglycerides, sudden discontinuation may exacerbate angina or cause MI

NMJ blocker

-Non-depolarizing NMJ blocker
-Relatively short acting

(Atropen, Atropisol)
Muscarinic receptor antagonist

-The major beladonna alkaloid

(Optivar, Astepro)
Topical Antihistamine use to treat allergic conjunctivitis or as a spray to treat allergic rhinitis and non-allergic vasomotor rhinitis

Centrally-acting skeletal muscle relaxant

-(GABA agonist)

-Bind allosterically to GABA-A receptor to potentiate its action
-Can directly stimulate the GABA-A receptor at high doses
-Able to reversibly depress all tissues in the body; CNS most sensitive
-Selective effects on reticular activating system and limbic system in CNS.
-Low therapeutic index
-Can increase reaction to pain (should not be used for pain management)
-Induces P450 -> Increased metabolism of vit. D, K, anticoagulants, and steroids
-Toxicity: depresses cardiac conduction
-Contraindicated in patients with porphyria - do not use in person with severe abdominal pain
-Enhances paralytic effect of turbocurare
-Other depressants enhance the CNS effects of barbiturates
Ester Local anesthetic

-Slow onset
-Short duration
-Moderate toxicity
-Topical anesthetic
-Rarely associated with methemoglobinemia
-Sedative and hypnotic
-High therapeutic index; does not depress respiratory drive or cardiovascular system
-Bind to γ subunit of GABA-A receptor and facilitate GABA mediated Cl- flux by increasing frequency of gating events
-Does not directly activate GABA-A receptor, even at high doses

-Effect: CNS depression up to coma
-Can depress hypoxic drive to breath at anesthetic doses -> respiratory acidosis in COPD patients
-Toxicity: Ataxia, confusion, amnesia; OD rarely fatal
-Toxicity can increase with age
-Dependance and abuse issues less of a problem than with EtOH and older sedatives

Muscarinic receptor antagonist

-(for treatment of Parkinson's disease)

Cholinergic agonist

-Synthetic derivative of ACh
-Muscarinic selective
-Not hydrolyzed by ChE

Direct Thrombin Inhibitor

-Direct, reversible thrombin inhibitor derived from leech anticoagulant protein
-Inactivates platelet bound Xa and clot bound thrombin

-Approved as IV anticoagulant to be used instead of heparin in patients with unstable angina undergoing percutaneous coronary intervention

-Does not cause immune thrombocytopenia (like heparin) and is not immunogenic (like lepuridin)

-Adverse Effect: bleeding (less than heparin though)
-As effective as UFH and safer for anticoagulation during PCI
-No antidote
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