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215 Cards in this Set

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Penicillin (MOA)
bind pbps, block transpeptidase cross-linking of cell wall, bacteria autolysin activity
Methicillin (toxicity)
interstitial nephritis
Ampicillin, Amoxicillin (clinical use)
Gram + and H. influenza, E. coli, Listeria, Proteus, Salmonella and enterococci
Ampicillin (toxicity)
pseudomembranous colitis
Ticarcillin, carbenicillin, pipercillin (clinical use)
Pseudomonas and gram - rods
B-lactamase inhibitors
clavulanic acid, sulbactam, tazobactam
Bacteriostatic
Erthromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol
Bacteriocidal
Vancomycin, Fluoroquinolones, Pencillin, Aminoglycosides, Cephalsporins, Metronidazole
Cephalosporins (MOA)
B-lactam drugs that inhibit cell wall synthesis but less suspectible to penicillins
1st generation Cephs (names and clinical use)
Cefazolin, Cephalexin
2nd generation Cephs (names)
Cefaclor, Cefoxitin, Cefuroxime, Cefamandole
2nd generation Cephs (clinical use)
HEN PEcKS
3rd generation Cephs
Ceftriaxone, Cefotaxime, Ceftazidine
4th generation Cephs
Cefepime
Cephs (toxicity)
Nephrotoxicity with aminoglycosides
Aztrenam (clinical use)
Gram - rods
Imipenem/cilastatin (MAO)
B-lactamase resistant carbapenem.
Imipenem and Meropenem (clinical use)
Broadest spectrum
Vancomycin (MAO and clinical use)
inhibits cell wall mucopeptide formation by binding D-ala D-ala
Vancomycin (Resistance)
amino acid change from D-ala to D-lac
Vancomycin (Toxicity)
Nephrotoxicity, Ototoxicity, Thrombophlebitis, RED MAN SYNDROME
30S inhibitors
Aminoglycosides
50S Inhibitors
Chloramphenicol, Clindamycin
Aminoglycosides (names and MAO)
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Aminoglycosides (clinical use and toxicity)
MUST HAVE OXYGEN--> ineffective against anaerobes
Aminoglycosides (resistance)
transferase enzyme or enzymes that inactivate by adenylation, acetylation, and phosphorylation
Tetracyclines (MAO)
prevent attachment of aminoacyl tRNA
Tetracyclines (clinical use)
Vibrio chlorea, acne, Chlamydia, Ureaplasma, Mycoplasma, H. Pylori, Borrelia, Rickettsia
Tetracylcine (toxicity)
teeth discoloration, inhibition of bone growth, photosensitivity
Macrolides (names and MAO)
ACE (azithromycin, clarithromycin, erythromycin)
Macrolides (clinical use)
Mycoplasma, Legionalla, Chlamydia, Neisseria
Macrolides (toxicity)
Prolonged QT interval, GI discomfort, acute cholestatic hepatitis
Chloramphenicol (MAO and clinical use)
inhibits 50S peptidyltransferase
Chloramphenicol (toxicity)
Aplastic anemia
Clindamycin (MAO)
blocks peptide bond formation at 50S ribosomal subunit
Drugs used for VRSA
Streptogramins (quinupristin/dalfopristin)
Sulfonamides (MAO)
PABA antimetabolite
Sulfonamides (toxicity)
hemolysis in G6PD deficiency
Trimethoprim (MAO and toxicity)
inhibits bacterial dihydrofolate reductase
Polymyxins (MAO)
bind to cell membranes of bacteria and disrupt their osmotic properties
Polymyxins (clinical use and toxicity)
used for resistant gram - infections
Ethambutol (MAO)
inhibits arabinosyl transferase which polymerizes arabinose into arabinoglactan
Ethambutol (toxicity)
red green color blindness
Rifampin (MAO)
inhibits DNA-dependent RNA polymerase
Rifampin (toxicity)
hepatotoxicity, P-450 inducers, orange body fluids
Tetracycline (resistance)
PUMP
Macrolides (resistance)
methylation of rRNA
Azoles (MAO)
inhibit fungal sterol synthesis (blocks 14-alpha-demethylase)
Flucytosine (MAO and toxicity)
inhibits DNA synthesis by conversion to 5-fluorouracil
Caspofugin (MAO and clinical use)
inhibits cell wall synthesis by inhibiting synthesis of B-glucan
Terbinafine (MAO and clinical use)
inhibits squalene epoxidase
Griseofulvin (MAO)
interferes microtubule function; disrupts mitosis
Griseofulvin (clinical use and toxicity)
dermatophytoses (oral treatment)
Amantadine (MAO)
blocks viral penetration/uncoating
Amantadine (clinical use and toxicity)
Influenza A and Parkinson's disease
Zanamivir, Oseltamivir (MAO)
inhibit influenza neuraminidase
Acyclovir (MAO)
Inhibits DNA synthesis in HSV, VZV, and EBV. Activated by viral thymidine kinase (TK- strains are resistant).
Acyclovir (toxicity)
crystalline nephropathy
Ganciclovir (MAO)
Inhibits DNA synthesis. Effective against herpes viruses CMV and HSV; for CMV requires bioactivation via viral phosphotransferase.
Ganiciclovir (toxicity)
leukopenia, neutropenia, thrombocytopenia, renal toxicity
Foscarnet (MAO)
Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase.
Foscarnet (clinical use and toxicity)
Uses: CMV retinitis in immunocomp pts. when gancyclovir fails. Tox: Nephrotoxicity
Protease Inhibitors (-navir) (MAO)
inhibit maturation of new virus by blocking protease in progeny virus
Protease Inhibitors (toxicity)
GI intolerance, hyperglycemia, kidney stones, thrombocytopenia
NRTI (names)
Zidovudine, Abacavir, Didanosine (ddI), Lamivudine (3TC), Stavudine (d4T), and Zalcitabine (ddC
NNRTI (names)
Efavirenz, Declaviridine, Nevirapine
Reverse transcriptase inhibitors (MAO)
inhibit reverse transcriptase of HIV
Reverse transcriptase inhibitors (toxicity)
bone marrow suppression, peripheral neuropathy, lactic acidosis (NRTI), rash (NNRTI)
Enfuviritide (MAO)
bind viral gp41 subunit
Maraviroc (MAO)
blocks CCR5 protein on T-cell surface to prevent viral entry
Interferons (MAO)
Glycoproteins synthesized by virus-infected cells block replication of both RNA and DNA viruses
Interferon alpha
used in hep B and C, kaposi's sarcoma
interferon beta
Multiple sclerosis
interferon gamma
NADPH oxidase deficiency
Praziquantel (MAO and clinical use)
Increases membrane permeability to Ca2+ causing muscle contraction followed by paralysis.
Ivermectin (MAO)
Intensifies GABA-mediated neurotransmission in nematodes, but no access to CNS in humans.
Mebendazole (MAO)
Inhibits microtubule synthesis and glucose uptake in
Sodium Stibogluconate (MAO)
Inhibits glycolysis at PFK reaction. Used against LESHMANIA DONOVANI.
Nifurtimox (MAO and clinical use)
Forms intracellular oxygen radicals, which are toxic to the organism. Used against TRYPANOSOMA CRUZI.
Cyclosporine (MAO)
inhibits calcineurin --> prevents production of IL-2 and its receptor
Cyclosporine (toxicity)
nephrotoxic, gingival hyperplasia, hirtuism
Tacrolimus (FK506) MAO
binds to FK-binding protein --> inhibiting secretion of IL-2
Azathioprine (MAO)
precursor of 6-mercaptopurine
Muromonab-CD3 (OKT3) MAO
monoclonoal antibody that binds to CD3 on the surface of T cells
Sirolimus (MAO
blocks tyrosine kinase. binds to mTOR.
Clinical use for Aldesleukin (interleukin2)
renal cell carcinoma
Clinical use for erythropoietin
Anemia esp in renal failure
alpha 1 receptor
increase vascular smooth muscle contraction, pupil dilator muscle (mydriasis), increase intestinal and bladder sphincter muscle contraction, decrease renin release
alpha 2 receptor
decrease insulin release, decrease sympathetic outflow
Beta 1 receptor (heart and kidney)
increase HR, contractility, renin release
Beta 2 receptor
vasodilation, bronchodilation, increase heart rate and contractility, increase insulin release, decrease uterine tone
M1
CNS
M2 (heart)
decrease HR and contractility of atria
M3 (peripheral)
increase exocrine gland secretions, miosis, accommodation
Bethanechol
Cholinomimetic. Activates bowel and bladder smooth muscle. Resistant to AChE. Uses: Postoperative and neurogenic ileus and urinary retention
Carbachol
Cholinomimetic. ACh analog. Uses: Glaucoma, pupillary constriction, and relief of intraocular pressure.
Pilocarpine
Cholinomimetic. Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle). Resistant to AChE. Uses: Glaucoma, Sjoren, Stimulator of tears, sweat, and saliva.
Neostigmine
Cholinesterase inhibitor. Increase endogenous ACh. Little CNS effect. Uses: Postoperative ileus and urinary retention, MG, reversal of neuromuscular blockade.
Physostigmine
Glaucoma, crosses BBB. atropine overdose
DUMBBELSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation.
Muscarnic antagonists
Atropine, Benztropine, Scopolamine, Ipratropium, Oxybutyin, Methscopalamine
Atropine
Blocks DUMBBELSS
Don't use Atropine in ...
acute angle glaucoma in elderly
Hexamethonium
Nicotinic antagonist (blocks para and sympathetic). Uses: Ganglionic blocker. In experimental models, prevents vagal reflex responses to changes in blood pressure - prevents reflex brady.
Hexamethonium (toxicity)
Tox: Orthostatic Hypotension, Blurred vision, constipation, sex dysfunction
Epinephrine (MAO)
Direct sympathomimetics. affinity for all receptors. low doses (B1), high doses (alpha1).
Epinephrine (clinical use)
anaphylaxis, glaucoma (open angle), asthma, hypotension
Epinephrine (toxicity)
tachycardia, hypertension, MI, pulmonary edema and hemorrhage
Norepinephrine (MAO)
Adrenoceptor agonist prototype: acts at B1- and all A adrenoceptors
Norepinephrine (clincal use and toxicity)
hypotension
Isopropterenol (low dose epi)
B1 and B2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, tremor, angina.
Dopamine
Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow (low dose) and positive inotropic effects (moderate dose).
Dobutamine
b1>b2
Dobutamine (clinical use)
shock, heart failure, cardiogenic shock
Phenylephrine
A1 > A2. Uses: Pupillary dilation, vasoconstriction, nasal decongestion
B2 selective agonist
Metaproterenol, Albuterol, Salmeterol, Terbutaline
Nonselective alpha blockers
Phenoxybenzamine (irreversible)
Prazosin, Terazosin, "-osins"
Alpha1-selective blocker prototype: used in HTN and benign prostatic hyperplasia. Tox: first-dose orthostatic hypotension but less reflex tachycardia than nonselective a blockers.
Alpha 2 blockers
Mirtazapine (depression) and Yohimbine
(Inducers) Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically
Quinidine, Barbiturates, St. John's wort, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, Chronic alcohol use
(Inhibitors) Inhibit yourself from drinking beer from a KEG because it makes you Acutely SICk
Sulfonamides, Isoniazid, Cimetidine, Ketoconazole, Erythromycin, Grapefruit juice, Acute alcohol use
HMG-CoA reductase inhibitors (MAO)
inhibit cholesterol precursor, upregulates LDL receptors
HMG-CoA reductase inhibitors (toxicity)
hepatitis
Niacin (MAO)
inhibits lipolysis in adipose tissue.
Niacin (toxicity)
flushed skin (decresed by aspirin)
Bile acid resins (cholestyramines)
Prevent intestinal reabsorption of bile acids. Liver must use cholesterol to make more
Bile acid resins (toxicity)
GI discomfort, decrease absorption of fat-soluble vitamins. GALLSTONES
Fibrates (MAO)
upregulate LPL--> increase in TG clearance
Fibrates (toxicity)
myositis
Hydralazine
Antihypertensive. Arteriolar vasodilator, orally active. Uses: Severe HTN, CHF, HTN in preg (with Methyldopa). Metabolized by Acetylation. Tox: Tachycardia, Salt and H2O retention, Lupus like syndrome.
Minoxidil
K+ channel opener that hyperpolarizes and relaxes vascular smooth muscle. Uses: Severe HTN, baldness. Tox: Hypertrychosis, Pericadial effusion, Reflex tachy, Angina, Salt retention.
Nifedipine
Dyhydropiridine calcium channel blocker. Vasoselective (N>D>V). Uses: Hypertension, Angina, Printzmetal's angina, Reynaud's. Tox: Cardiac depression, AV block, edema, flushing, dizziness, constipation.Others: Amlodipine (HF), Nimodipine (subarachnoid hemmorhage), Nicardipine
Fenoldopam
D1 receptor antagonist. Relaxes smooth muscle. Powerful vasodilator. Uses: Hypertensive emergencies
Digoxin
Cardiac glycoside. Direct inhibitor of Na+/K+ pump leading to indirect inhibition of Na+/Ca++ exchanger and increasing intracellular calcium levels. Stim. vagus. T1/2 40hrs. Uses: CHF, A-fib. Tox: Calcium overload arrhythmias, GI upset.
Quinidine, Procainamide, Disopyramide
. Uses: Atrial and vetricular arrhythmias. Tox: Cinchonism - headache, tinnitus, Thrombocytopenia, Torsades. Others: Procainamide, Dysopyramide. Increase AP
Lidocaine, Mexiletine, Tocainide
Selectively affects ischemic or depolarized vent. tissue. Uses: Acute V-arrhythmias (post MI) and digoxin tox. Tox: Local anesthetic, CNS stim/ dep, cardiovascular depression. Others: Mixeiletine (Oral), Tocainide. Decrease AP
Flecainide, Encainide, Propafenone
Class 1C antiarrhythmic. No effect on AP. Uses: V-tach and rapid SVT with WPW. Tox: Proarrhythmic (post MI), Prolongs refractory period in AV. Others: Encainide, Propafenone
Adenosine
Unclassified antiarrhythmic. Parenteral only. Hyperpolarizes AV nodal tissue causing block for 10 - 15 secs. Very short acting. Uses: Drug of choice in abolishing/ diagnosing SVT. Tox: flushing, hypotension, chest pain
Mg++
Effective in torsades de pointes and digoxin toxicity.
Lispro, Aspart, Regular Insulin
Short acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
NPH
Intermediate acting insulin analog. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
Glargine, Detemir
Long acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia
Sulfonlyureas
Blocks K+ channels in pancreatic B cells, causing depolarization and release of insulin. Uses: Only DM2. Tox: hypoglycemia, weight gain, cholestatic jaundice
Metfomin
Oral biguanide hypoglycemic. Decreases hepatic gluconeogenesis, Increase Glycolysis, and peripheral glucose uptake (insulin sensitivity). Uses: Oral, can be used in DM1. Minimal hypoglycemia or weight gain. Tox: Lactic acidosis. DON'T use in renal failure
Pioglitazone, Rosiglitazone
peroxisome proliferator-activator receptors (PPARs) enhances target tissue sensitivity to insulin.
Acarbose, Miglitol
Alpha-glucosidase inhibitors. Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia. Uses: DM2. Tox: GI disturbances.
Pramlintide
Mimetic.(amylin analog) Decreases glucagon release. Uses: DM2. Tox: Hypoglycemia, nausea, diarrhea
Exenatide
GLP-1 analog. Increased insulin, decreased glucagon release. Uses: DM2. Tox: Nausea vomiting, pancreatitis, weight loss
Propylthiouracil, Methimazole
Antithyroid drug. Inhibits tyrosine iodination and coupling reactions. Orally active. Uses: Hyperthyroidism. Tox: Rash, agranulocytosis (rare). Methimazole is a possible teratogen
Levothyroxine, triodothyronine
Thyroid replacement. Uses: Hypothyrodism, myxedema. Tox: Tachycardia, heat intolerance, tremors, arrhythmias.
Glucocorticoids
Decrease production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX2. Uses: Addisons disease, inflammation, immune suppression, asthma. Tox: Cushing's syndrome. Adrenal insufficiency when drug is stopped after chronic use.
Bismuth, Sulfralfate
Binds to ulcer base, provides physical protection, and allows HCO3- secretion to establish pH gradient in mucous layer. Uses: Ulcer healing and traveler's diarrhea.
Misoprostol
PGE1 analog. Increased production of mucus and decreased acid secretion
Antacids
Can affect absorption, bioavailability, or excretion of other drugs due to alteration of gastric/ urine pH. Tox: Aluminum Hyd.- conspitation, Mag Hyd. - Diarrhea, Cacium Carb - Hypercalcemia. All can cause hypokalemia.
Sulfasalazine
A combination of Sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflammatory). Activated by colonic bacteria. Uses: UC, Crohn's. Tox: Malaise, nausea, sulfonamide toxicity, reversible oligospermia.
Metaclopramide
D2 receptor antagonist. Increase resting tone, contractility, LES tone, motility. Uses: Diabetic and post-surgery gastroparesis. Tox: Parkinsonian effects, Restlessness, Drowsiness, Drug interactions with Digoxin and diabetic agents.
Dimercaprol
chelating agent used in treatment of arsenic poisoning by displacing arsenic ions from sulfhydryl
Streptokinase
Thrombolytic. Protein from streptococci that accelerates
Alteplase
Thrombolytic. Human recombinant tissue plasminogen
Clopidogrel
Blocks platelet ADP receptors irreversibly and inhibits platelet
Brimonidine
Alpha agonist used in Glaucoma. Decrease aqueous humor synthesis. No pupillary or visual changes.
B- blockers: Timolol, betaxolol, carteolol
Decrease aqueous humor synthesis. No pupillary or visual changes.
Latanoprost
Prostaglandin used in Glaucoma. Increase outflow of aqueous humor. Tox: Darkens color of iris (browning)
Opioid Analgesics (MAO)
agonists at opoid receptors to modulate synaptic transmission-- open K+ channels, close Ca2+ channels --> decrease synaptic transmission
Opioid Analgesics (Clinical use)
Pain, cough suppression (dextromethorphan), diarrhea (loperamide and diphenoxylate), maintence program for addicts
Opioid Analgesics (Toxicity)
respiratory depression, pinpoint pupils, CNS depression
Butorphanol
Partial agonist at opioid mu receptors, agonist at kappa receptors. Uses: Pain, causes less resp. depression than full agonists. Tox: Causes withdrawal if on full opioid agonist.
Tramadol (MOA)
inhibits NE and serotonin reuptake (works at multiple receptors)
Phenytoin (MAO)
Anticonvulsant. Used for tonic-clonic and partial seizures;
Phenytoin (toxicity)
sedation, diplopia, gingival
Barbiturates (MAO)
Facilitate GABA by increasing DURATION of Cl- channel opening --> decrease neuron firing
Barbiturate (clinical use)
sedative for anxiety, seizures, insomia
Barbiturate (toxicity)
additive CNS depression with alcohol, respiratory and CV depression. Induction of P450
Gabapentin
Anticonvulsant: structural analog of GABA that facilitates its
Lamotrgine
Newer antiepiliptic drug for absence and partial seizures; also
Carbamazepine
Anticonvulsant: used for tonic-clonic and partial seizures;
Valproic acid
Anticonvulsant: primary drug in clonic-tonic, absence, and
Ethosuximide
Anticonvulsant: primary in absence seizures; may block T-type Ca2+ channels in thalamic neurons. Tox: GI distress; safe in
Baclofen (MOA)
binds to GABAb. increase K+ efflux. hyperpolarization
Benzo's (MAO)
Facilitate GABAa action by increasing FREQUENCY of Cl- channel opening. decrease REM sleep
Benzo's (clinical use)
anxiety, spastic, status epilepticus, detox, night terrors and sleepwalking
Benzo's (toxicity)
treat overdose with Flumazenil
Vigabatrin
Anticonvulsant. Irreversibly inhibits GABA transaminase - increase in GABA.
Halothane
General anestheti. Inhaled halogenated hydrocarbon. Tox: cardiovascular and respiratory depression and relaxation of skeletal and smooth muscle. Use is declining because of sensitization of heart to catecholamines and occurrence (rare) of hepatitis. Others: Fluranes + NO.
Midazolam
Most common drug used for endoscopy. Used adjuntively with gaseous anesthetics and narcotics. May cause severe postoperative respiratory depression, decrease in BP, and amnesia.
Ketamine
PCP analog that acts as dissociative anesthetic. Block NMDA receptors. Cardovascular stimulant. Cause disorientaion, hallucination, and bad dreams. Increase cerebral blood flow.
Succinylcholine
Depolarizing neuromuscular relaxant. Short duration
Tubocurarine
Nondepolarizing neuromuscular blocking agent. Competitive nicotinic blocker (ACh). Releases histamine and may cause hypotension. Analogs: pancuronium, atracurium, vecuronium, and other "-curiums" and "-oniums." Tox: respiratory paralysis. Antidote: cholinesterase inhibitor, eg, neostigmine.
Dantrolene (clinical use)
used in treatment of malignant hyperthermia and to treat neuroleptic malignant syndrome
Dantrolene (MAO)
prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle by blocking ryanodine receptors
Agonize dopamine receptors
Bromocriptine, pergolide, pramipexole, ropinirole
Prevent dopamine breakdown
Selegine (MAO type b inhibitor)
l-dopa
Dopamine precursor: used in parkinsonism, usually combined
Memantine
Alzheimers drug. NMDA receptor antagonist; Helps prevent excitotoxicity (mediated by Ca++). Tox: Dizziness, confusion, hallucinations
Donepezil
Alzheimers drug. Acetylcholinesterase inhibitors. Tox: Nausea, vomiting, insomnia.
Huntington drugs
Reserpine + tetrabenazine - amine depleting. Haloperidol - dopamine receptor antagonist. Dz - Increase dopamine, decrease GABA + ACh.
Sumatriptan
5-HT1D receptor agonist: used to abort migraine attacks. Tox:
Haloperidol + azines
Antipsychotic: blocks brain dopamine D2 receptors (Increase cAMP). Uses: Schizophrenia, Psychosis, Acute mania, Tourette's. Tox: marked EPS dysfunction (Hal, Flu drugs), hyperprolactinemia; neuroleptic malignant syndrome, tardive dyskinesia
NMS
FEVER
Tardive dyskinesia
Sterotypic oral-facial movements due to long-term antipsychotic use. Often irreversible
Olanzapine
Atypical antipsychotic; high-affinity antagonist at 5-HT2 receptors with minimal extrapyramidal side effects; improves
Clozapine
Atypical antipsychotic: low affinity for dopamine D2 receptors, higher for D4 and 5-HT2A receptors; fewer EPS adverse
Lithium
Antimanic prototype: a primary drug in mania and bipolar affective disorders; blocks recycling of the phosphatidylinositol
Buspirone
Anxiolytic: partial agonist that interacts with 5-HT1A receptors; slow onset (1-2 weeks). Uses: GAD. Minimal potentiation of CNS depressants, including ethanol; negligible abuse liability.
TCAs (Imipramine, Amytriptyline, Clomipramine, Doxepin)
blocks reuptake of norepinephrine and serotonin. Uses: Major depression, bedwetting (Imi), OCD (Clop), fibromylagia.
TCAs (toxicity)
atropine-like, postural hypotension, sedation, cardiac arrhythmias in overdose, additive effects with other CNS depressants. 3-C: Convulsions, Coma, and Cardiotox.
SSRIs (Fluoxitine, Paroxitine, Sertaline, Citalopram) (MAO and clinical use)
selective serotonin reuptake inhibitor
SSRI (toxicity)
Tox: CNS stimulation, sexual dysfunction, seizures
Venlafaxine, Duloxetine
Serotonin and NE reputake inhibitors. Uses: Depression. Venla - GAD. Dulo - Diabetic peripheral neruopathy. Tox: Hypertension
Phenelzine, Tranylcypromine, Isocarboxazid (MAO and clinical use)
Irreversible nonselective monoamine oxidase (MAO) inhibitor. Increases level of neurotransmitters. Uses: backup drug for atypical depression, hypochondrias
Phenelzine, Tranylcypromine, Isocarboxazid (toxicity)
Tox: malignant hypertension with indirect-acting sympathomimetics and tyramine, serotonin syndrome with serotonergic drugs.
Selegiline
MAO-B inhibitor: selective inhibitor of the enzyme that metabolizes dopamine (no tyramine interactions). Uses: Parkinson's disease. Tox: GI distress, CNS stimulation, dyskinesias, serotonin syndrome if used with selective serotonin reuptake inhibitors.
Bupropion
Atypical antidepressant. Used in smoking cessation. Increases NE and dopamine via unknown mech. Tox: Stimulant effect, headache, seizure in bulemic patients.
Mirtazapine
Atypical antidepressant. Alpha 2 agonist (increase release of NE + Ser) and potent Serotonin receptor antagonist. Used in anorexia. Tox: Sedation, Increased appetite, weight gain, ortho hypotension.
Trazodone
Atypical antidpressant. Primarily inhibits serotonin reuptake. Used for insomnia, as high doses are needed for anti-depressant effects. Tox: Sedation, nausea, priapism, postural hypotension