Pharmacology Flashcards by Joyce Ann Garcia

rapidly hydrolyzed by AChE

Acetylcholine (TOPNOTCH)

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resistant to AChE

Betanechol (TOPNOTCH)

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for Bladder and bowel atony

Betanechol (TOPNOTCH)

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Nonselective muscarinic and nicotinic agonist , used topically for glaucoma treatment

Carbachol (TOPNOTCH)

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Partial muscarinic agonist; used for treatment of Glaucoma, Sjogren’s syndrome and Sicca syndrome

Pilocarpine (TOPNOTCH)

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Adverse Effects of Acetylcholine

CNS stimulation, miosis, cyclospasm, brochoconstriction, excessive GI and GU smooth muscle contraction, increased secretory activity of sweat gland, airways etc, vasodilation (TOPNOTCH)

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activates autonomic post ganglionic neurons (both sympathetic and parasympathetic) and skeletal muscle neuromuscular end plants

Nicotine(TOPNOTCH)

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used exclusively for smoking cessation

Varenicline (TOPNOTCH)

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for Myasthenia gravis diagnosis (Tensilon test)

Edrophonium (TOPNOTCH)

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for Myasthenia gravis treatment; reversal of nondepolarizing muscular blockade

Neostigmine (TOPNOTCH)

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Long Acting Cholinesterase Inhibitors used as Scabicide and Insecticide

Malathion, Parathion (TOPNOTCH)

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Competitively blocks all muscarinic receptors, antagonizes histamine and serotonin ; for motion sickness, dec. acid secretion in the GIT

Scopolamine (TOPNOTCH)

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DOC for organophosphate poisoning

Atropine (TOPNOTCH)

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for bradycardia, hypersalivation and to decrease airway secretion during general anesthesia

Atropine (TOPNOTCH)

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Mydriatic, cycloplegic in eye examinations

Homatropine, Cyclopentolate, Tropicamide (TOPNOTCH)

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Competitive nonselective antagonist at muscarinic receptors ; for BA and COPD, not as effective as SABAs but less tachycardia and arrhythmia

Ipratropium, Tiotropium (TOPNOTCH)

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Nonselective muscarinic antagonist which reduces detrussor smooth muscle tone spasms

Oxybutinin (TOPNOTCH)

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for decreasing urgency in mild cystitis and dec. bladder spasm after urologic surgery

Oxybutinin (TOPNOTCH)

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Usual antidote for early stage (48h) cholinesterase inhibitor poisoning, Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs

Pralidoxime (TOPNOTCH)

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Competitively blocks all Nn nicotinic Ach receptors ; for Hypertensive emergencies (obsolete)

Hexamethonium, Mecamylamine, Trimethaptan (TOPNOTCH)

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DOC for Anaphylaxis

Epinephrine (TOPNOTCH)

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used for Cardiac arrest, anaphylaxis, asthma, COPD, Hemostasis

Epinephrine (TOPNOTCH)

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for cardiogenic Shock and heart failure

Norepinephrine (TOPNOTCH)

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causes vasodilation in splanchnic and renal blood vessels ; for cardiogenic Shock and heart failure

Dopamine (TOPNOTCH)

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Beta nonselective sympathomimetic, for Asthma

Isoproterenol (TOPNOTCH)

SE: Rebound nasal congestion, hypertension, stroke, MI

Phenylephrine (TOPNOTCH)

A2 agonist, for Hypertension, Cancer pain, opioid withdrawal

Clonidine (TOPNOTCH)

Sedation, rebound hypertension, dry mouth

Clonidine (TOPNOTCH)

Sedation, positive Coomb's test (Hemolytic anemia)

Methyldopa (TOPNOTCH)

A2 agonist; reserved for ophthalmologic use in glaucoma for reduction of intraocular pressure

Apraclonidine, Brimonidine (TOPNOTCH)

B1 agonist, for cardiogenic shock and acute heart failure

Dobutamine (TOPNOTCH)

DOC as Asthma reliever, Rapid development of tolerance

Albuterol/Salbutamol (TOPNOTCH)

D1 agonist, for Hypertension

Fenoldopam (TOPNOTCH)

D2 agonist, restores dopamine actions in the CNS for Parkinson's disease, prolactinemia

Bromocriptine (TOPNOTCH)

Irreversibly blocks A1 and A2 receptors resulting to indirect baroreflex activation

Phenoxybenzamine (TOPNOTCH)

Reversible A1 and A2 receptor antagonist, for Pheochromocytoma and Rebound hypertension

Phentolamine (TOPNOTCH)

Blocks A1, for Benign Prostatic Hyperplasia, Hypertension

Prazosin, Doxazosin, Terazosin (TOPNOTCH)

Slightly selective A1a blockade causing relaxation of prostatic smooth muscles > vascular smooth muscle ; for BPH

Tamsulosin (TOPNOTCH)

Beta blockade > A1 blockade

Labetalol (TOPNOTCH)

Blocks B1 and B2 receptors

Propranolol, Nadolol, Timolol (TOPNOTCH)

B1 > B2 blockade

Metoprolol, Atenolol, Alprenolol, Betaxolol, Nebivolol (TOPNOTCH)

B1, B2 with intrinsic sympathomimetic (partial agonist) effect

Pindolol, Acebutolol, Carteolol, Bopindolol, Oxprenolol, Celiprolol, Penbutolol (TOPNOTCH)

Beta blockade > A1 blockade

Carvedilol, Medoxalol, Bucindolol, Labetalol (TOPNOTCH)

B1 > B2 blockade; for rapid control of BP and arrhythmias, thyrotoxicosis and myocardial ischemia intraoperatively ; for Supraventricular tachycardia

Esmolol (TOPNOTCH)

BB with direct vasodilating effect

Nebivolol (TOPNOTCH)

BB with local anesthetic effect

Propranolol (TOPNOTCH)

BB which is safe in pregnant patients

Labetalol (TOPNOTCH)

Mydriasis without cycloplegia

Phenylephrine (TOPNOTCH)

Cholinesterase Inhbitors with poor lipid solubility, oral, DOA: 30min-2h

Neostigmine (TOPNOTCH)

lower BP by decreasing volume

Diuretics (TOPNOTCH)

Inhibit NA/CL transporter in distal convoluted tubule

Thiazide Diuretics (TOPNOTCH)

for mild to moderate hypertension(first line), Heart falure, Nephrogenic Diabetes Insipidius, Renal calcium stones

Thiazide Diuretics (TOPNOTCH)

Thiazide Diuretics

HCTZ, Chlorthalidone, Metolazone, Indapamide (TOPNOTCH)

hyperlipidemia, hyperuricemia, sulfa allergy, hyperglycemia, hypercalcemia

HCTZ, Chlorthalidone, Metolazone, Indapamide (TOPNOTCH)

Inhibit NA/K/2Cl transporter in thick ascending limb of loop of Henle

Loop Diuretics (TOPNOTCH)

Loop Diuretics

Furosemide, Torsemide, Bumetanide, Ethacynic Acid (TOPNOTCH)

Hypokalemic metabolic alkalosis, Potassium wasting, ototoxicity, hyperuricemia, nephrotoxicity, dehydration, hypomagnesemia,sulfa allergy, hypocalcemia

Loop Diuretics (TOPNOTCH)

activates a2 adrenergic receptors ; for hypertensive urgency

Clonidine (TOPNOTCH)

activates a2 adrenergic receptors, for pre eclampsia

Methyldopa (TOPNOTCH)

Taper use prior to discontinuation to avoid rebound hypertension ; readily enter the CNS

Clonidine (TOPNOTCH)

Irreversibly blocks the vesicular monoamine transporter(VMAT)

Reserpine (TOPNOTCH)

Block release of NE from the pre-synaptic neuron

Guanethidine, Guanadrel (TOPNOTCH)

alpha-1 blocker which is most selective for prostatic smooth muscle

Tamsulosin (TOPNOTCH)

Disadvantage of Prazosin compared to other alpha-1 blockers

short DOA (TOPNOTCH)

Release NO from endothelial cells, Relaxes arteriolar smooth muscle, causing vasolidation. Decreases afterload ; for pre-eclampsia, hypertension, heart failure

Hydralazine (TOPNOTCH)

drug induced lupus (hydralazine), reflex tachycardia

Hydralazine (TOPNOTCH)

Opens K+ channels in vascular smooth muscle, causing hyperpolarization, muscle relaxation and vasolidation

Minoxidil, Diazoxide (TOPNOTCH)

for alopecia / male pattern baldness, hypertension

Minoxidil (TOPNOTCH)

Constipation, Nausea, flushing,gingival hyperplasia, AV block, sinus node depression, Pretibial edema, dizziness

Non-dihydropyridine calcium channel blocker: Verapamil, Diltiazem (TOPNOTCH)

block voltage-gated L-type calcium channels (vascular > cardiac); for Angina, hypertension

Dihydropyridine calcium channel blocker: Nifedipine, Amlodipine, Nicardipine, Nisoldipine, Isradipine, Felodipine (TOPNOTCH)

relaxes venous and arteriolar smooth muscle

Nitroprusside (TOPNOTCH)

for acute heart failure, controlled hypotension, cardiogenic shock, hypertensive emergency

Nitroprusside (TOPNOTCH)

a thiazide derivative without a diuretic effect ; also induces insulin release (can be used to treat hypoglycemia in insulin-producing tumors)

Diazoxide (TOPNOTCH)

causes arteriolar vasolidation of the afferent and efferent arterioles

Fenoldopam (TOPNOTCH)

inhibit angiotensin converting enzyme ; for hypertension, heart failure

ACE inhibitors: Captopril, Enalapril, Lisinopril, Benazepril (TOPNOTCH)

slows down the progression of DM nephropathy and cardiac remodelling in heart failure

ACE inhibitors: Captopril, Enalapril, Lisinopril, Benazepril (TOPNOTCH)

competetively blocks Angiotensin 1 receptor site ; for hypertension

Angiotensin receptor blocker: Losartan, Valsartan, Irbesartan, Candesartan (TOPNOTCH)

inhibitor of renin's action on its substrate angiotensinogen

Aliskerin (TOPNOTCH)

releases nitric oxide(NO), relaxes smooth muscle, especially vascular, increases Cgmp (cyclic guanosine monophosphate); for cyanide poisoning

Amyl Nitrite (TOPNOTCH)

releases nitric oxide (NO), increases Cgmp (cyclic guanosine monophosphate) and relaxes smooth muscle especially vascular; for Angina, acute coronary syndromes

Nitroglycerin, Isosobide Dinitrate, Isosobide Mononitrate (TOPNOTCH)

Dangerous hypotension with PDE inhibitors

Nitroglycerin, Isosobide Dinitrate, Isosobide Mononitrate (TOPNOTCH)

block voltage-gated L-type calcium channels (cardiac > vascular); for Angina, Supraventricular tachycardia, migraine, hypertension

Non-dihydropyridine calcium channel blocker: Verapamil, Diltiazem (TOPNOTCH)

inhibits Na/K ATPase; increases intracellular Ca, increasing cardiac contractility; for heart failure, Nodal arrythmias

Digoxin (TOPNOTCH)

Arrythmogenesis increased hypokalemia, hypercalcemia, hypomagnesemia

Digoxin (TOPNOTCH)

Hyperkalemia exacerbates cardiac toxicity

Class 1 Antiarryhtmics (TOPNOTCH)

Prolong AP duration

Class 1A: Procainamide, Disopyramide, Quinidine (TOPNOTCH)

Shorten AP Duration

Class 1B: Lidocaine, Mexiletene, Tocainide, Phenytoin (TOPNOTCH)

No effect on AP Duration

Class 1C: Flecainide, Propafenone, Encainide, Moricizine (TOPNOTCH)

Group with the greatest risk for TDP

Class 3 Arryhytmics (TOPNOTCH)

for Post MI prophylaxis against sudden death, thyrotoxicosis, acute perioperative and thyrotoxic arrythmias, Supraventricular tachycardia

Class 2: Propranolol, Esmolol (TOPNOTCH)

has Class 1, 2 3 and 4 activity therefore is the MOST EFFICACIOUS of all anti-arrhythmics

Amiodarone (TOPNOTCH)

DOC for paroxysmal supraventricular tachycardia

Adenosine (TOPNOTCH)

for glaucoma, diuresis for edema with alkalosis.

Carbonic Anhydrase Inhibitors (TOPNOTCH)

Carbonic Anhydrase Inhibitors

Acetazolamide, Dorzolamide, Brinzolamide, Dichlorphenamide, Methaolamide (TOPNOTCH)

Efficacy decreasedby NSAIDs

Loop Diuretic, Thiazide Diuretics (TOPNOTCH)

For hypertension Hypercalciuria, Heart failure, Nephrogenic diabetes insipidius, renal calcium stones

Thiazide Diuretics: Hydrochlorothiazide, Chlorthalidone, Indapamide, Metolazone (TOPNOTCH)

Cause powerful diuresis and increased Ca excretion

Loop Diuretic: Furosemide, Bumetanide, Torsemide (TOPNOTCH)

Steroid inhibitors of cytoplasmic aldosterone receptor in cortical collecting ducts. Reduce K excretion;

Spironolactone, Eplerenone(Aldosterone Antagonist) (TOPNOTCH)

Inhibitor of ENaC (Epithelial sodium channels) in cortical collecting duct, reduces Na reabsorption and K excretion; for hypokalemia

Amiloride, Triamterene (TOPNOTCH)

reduces progression of DM nephropathy and reduces mortality post MI

Eplerenone (TOPNOTCH)

Osmotic Diuretics

Mannitol, Glycerin, Isosorbide, Urea (TOPNOTCH)

Transient volume expansion (hyponatremia, pulmonary edema; followed by hypernatremia) nausea, headache, dehydration, vomiting

Osmotic Diuretics SE (TOPNOTCH)

Agonists at V1 and v2 ADH receptors. Activate insertion of aquaporin water channels in collecting tubule.

Antidiuretic hormone, Desmopressin (TOPNOTCH)

Antagonist at V1a, V2 receptors; for SIADH and Hyponatremia

Conivaptan, Tolvaptan, Lixivaptan (TOPNOTCH)

more likely to block autonomic receptors, also has alpha1 blocking and local anesthetic effect

1st Generation antihistamines (TOPNOTCH)

Reversible blockade of histamine H1-receptor sites on tissues, No sedation and antimuscarinic effects

2nd Generation antihistamines (TOPNOTCH)

may cause arrhythmia due to blockade of cardiac potassium channels

acrivastine, astemizole, cetirizine, loratadine, and terfenadine (TOPNOTCH)

reduction of nocturnal acid secretion in gastirc and duodenal ulcer

H2 antagonists (TOPNOTCH)

True or False: H2 antagonists have H1-blocking effect

FALSE (TOPNOTCH)

True or False: Ranitidine is a CYP450 inhibitor

TRUE, but weak inhibitor only (TOPNOTCH)

Agonist at the 5HT1D receptor in the blood vessels causing vasocontriction ; 1st line treatment for Acute migraine and cluster headache attacks

5HT1D receptor agonist: Sumatriptan, Naratriptan, Almotriptan, Eletriptan, Frovatriptan, Rizatriptan, Zolmitriptan (TOPNOTCH)

Selectively block 5HT3 receptors ; For antiemesis in patients post-chemotherapy or post-operation

5HT3 receptor antagonist: Ondansetron, Granisetron, Dolasetron, Alosetron (TOPNOTCH)

can inc QRS and QT (proarrhythmic effect) duration so never use in patients with heart disease

Dolasetron (TOPNOTCH)

SE: gangrene (sec to Ischemia) in overdose, unusual hyperplasia of the retroperitoneal, retropleural or subendocardial cavity --> hydronephrosis, cardiac valvular and conduction system malfunction

Ergotamine (TOPNOTCH)

uterus becomes more sensitive to ergots during pregnancy, produce very powerful and long-lasting contraction leading to decreased bleeding, Never give before delivery of placenta

Ergonovine (TOPNOTCH)

PGE1 analogue, causes increased HCO3 and mucus secretion in stomach and uterine contraction

Misoprostol, Gemeprost (TOPNOTCH)

may also be used together with Mifepristone or Methotrexate as safe abortifacient

Misoprostol (TOPNOTCH)

Low concentrations contract, higher concentrations relax uterine and cervical smooth muscle, soften cervix at term before induction with oxytocin

Dinoprostone, Sulprostone (TOPNOTCH)

PGF2a analogue, increases outflow of aqueous humor thus reduces intraocular pressure; For glaucoma

Prostaglandin F2a analog: Latanoprost, Arboprost, Bimatoprost, Travoprost, Unoprostone (TOPNOTCH)

used primarily for pulmonary hypertension

Prostaglandin I2 analog: Epoprostenol, Beraprost, Iloprost, Treprostinil (TOPNOTCH)

SE: Tachycadia, Nervousness, tremors, restlessness, arrythmias when used excessively, loss of responsiveness (tolerance, tachyphylaxis)

Beta2-selective agonist (short-acting): Albuterol/Salbutamol, Levalbuterol, Terbutaline, Metaproterenol, Pirbuterol, Procaterol, Fenoterol (TOPNOTCH)

Increase asthma mortality when used alone; May precipitate arrhytmias; usual DOA: 12hrs

Beta2-selective agonist (long acting): Salmeterol, Formoterol, Cleneterol, Bambuterol (TOPNOTCH)

More effective and less toxic than beta agonists ith COPD

Muscarinic receptor antagonist: Ipratropium, Tiotropium (TOPNOTCH)

Phosphodiesterase inhibitor, Adenosine receptor antagonist, causes bronchodilation and inc. strength of contraction of diaphragm; For asthma esp in nocturnal attacks

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

Antidote in overdosage is BB. Higher clearance in adolescents and smokers. Narrow therapeutic window

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

Prevents calcium influx and stabilizes mast cells, preventing degranulation and release of histamine, leukotrienes and mediators; for Asthma prophylaxis and allergies

Mast cell Stabilizer: Cromolyn, Nedocromil, Lodoxamide (TOPNOTCH)

DOC for Asthma prophylaxis, First line treatment for moderate to severe BA, COPD

Corticosteroid: Fluticasone, Beclomethasone, Budesonide, Flunisolide, Mometasone, Triamcinolone, Ciclosenide (TOPNOTCH)

For status asthmaticus

use IV prednisolone or hydrocortisone (TOPNOTCH)

active metabolite of prednisone

prednisolone (TOPNOTCH)

Inhibitor of 5-lipoxygenase. Reduces synthesis of leukotrienes. Prevents airway inflammation and bronchoconstriction; For asthma prophylaxis

Zileuton (TOPNOTCH)

No bronchodilator action, not recommended for acute BA attack

Zileuton, Montelukast, Zafirlukast, Pranlukast (TOPNOTCH)

Binds IgE antibodies on sensitized mast cells and prevents activation by BA triggers and subsequent release of inflammatory mediators; For prophylaxis of severe, refractory asthma not responsive to all other drugs

Anti-IgE antibody: Omalizumab (TOPNOTCH)

bind GABA-A receptor subunits to increase frequency of chloride channel opening which causes membrane hyperpolarization

benzodiazepines (TOPNOTCH)

SE: anterograde amnesia, decreased psychomotor skills, unwanted daytime sedation, tolerance, dependence liability and rebound insomnia or anxiety

benzodiazepines (TOPNOTCH)

BZD that can be used for seizure disorders, Bipolar disorder and infantile spasm

Clonazepam (TOPNOTCH)

Why is Lorazepam preferred over Diazepam in status epilepticus

due to its long distribution halflife (TOPNOTCH)

date-rape drug

Flunitrazepam (TOPNOTCH)

BZD used for alcohol withdrawal

Diazepam and Chlordiazepoxide (TOPNOTCH)

antagonist at benzodiazepine sites on GABA-A receptor

Flumazenil (TOPNOTCH)

bind to GABA-A receptor sites to increase duration of chloride channel opening, block glutamic acid neurotransmission

barbiturates (TOPNOTCH)

which has greater dependence liability: barbiturates or benzodiazepine

barbiturates (TOPNOTCH)

Barbiturate with the highest lipid solubility

Thiopental (TOPNOTCH)

barbiturate for status epilepticus

Phenobarbital (TOPNOTCH)

SE: acute intermittent porphyria

barbiturates (TOPNOTCH)

High dose BZD and Barbs may suppress seizure but at the expenses of marked sedation EXCEPT for

Clonazepam and Phenobarbital (TOPNOTCH)

only interact with GABA-A receptors with alpha-1 subunit; For insomnia and sleep disorder esp when sleep onset is delayed

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

dependence liability and withdrawal symptoms is less than that of benzodiazepines

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

lack anti-convulsant, anti-anxiety and muscle relaxant effects, effects are reversed with Flumazenil, very rapid onset of action, may dec REM sleep

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

increasing use due to rapid onset with minimal effects on the sleep pattern and cause less daytime cognitive impairment as compared to BZD

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

partial agonist at 5-HT1A receptors and possibly D2 receptors, used For generalized anxiety disorders

Buspirone (TOPNOTCH)

slow onset of action (more than 1week), metabolized by CYP3A4, safe for pregnant patients

Buspirone (TOPNOTCH)

activates melatonin receptors (MT1 and MT2 receptors) in the suprachiasmatic nuclei in the CNS leading to dec latency of sleep onset

Ramelteon (TOPNOTCH)

block voltage-gated Na channel; DOC for generalized tonic-clonic seizures, DOC for partial seizures, can be used for migraine

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

SE: nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal hydantoin syndrome, abnormalities in Vit D metabolism

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

preferred in prolonged therapy for status epilepticus because it is less sedating

phenytoin (TOPNOTCH)

block voltage-gated Na channels and decreases glutamate release; DOC for trigeminal neuralgia, DOC for generalized tonic-clonic seizures, DOC for partial seizures, for bipolar disorders

Carbamazepine, Oxcarbazepine (TOPNOTCH)

SE: diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, Stevens-Johnson syndrome, erythematous rash, teratogen (spina bifida and craniofacial anomalies), hyponatremia

Carbamazepine, Oxcarbazepine (hyponatremia) (TOPNOTCH)

may be used for acute manic phase and as prophylaxis in the depressive phase

Carbamazepine, Oxcarbazepine (TOPNOTCH)

blocks high-frequency firing of neurons which modifies amino acid metabolism; DOC for bipolar disorder (acute mania), DOC for generalized tonic-clonic seizures and absence seizure, partial seizures, myoclonic seizures, also used for Bipolar disorders

Valproic acid (TOPNOTCH)

anti-manic that is CYP450 inhibitor

Valproic acid (TOPNOTCH)

for status epilepticus in children ; primary anticonvulsant in infants, children and pregnant patients

Phenobarbital (TOPNOTCH)

inhibit low threshold (T-type) Ca currents esp in thalamic neurons ; DOC for absence seizure

Ethosuximide, Phensuximide, Methsuximide (TOPNOTCH)

blocks Ca channels, increases GABA release ; For neuropathic pain such as postherpetic neuralgia, partial seizures, migraine

Gabapentin, Pregabalin (TOPNOTCH)

structural analogues of GABA but does not activate GABA receptor directly ; also have the same effect on Ca currents like Ethosuximide

Gabapentin, Pregabalin (TOPNOTCH)

blocks Na and Ca channels and decreases glutamate, used for acute manic phase and as prophylaxis in the depressive phase

Lamotrigine (TOPNOTCH)

primarily undergoes glucuronidation reaction ; SE: dizziness, ataxia, nausea, rash, SJS / TEN

Lamotrigine (TOPNOTCH)

Bind synaptic protein selectively inhibiting hypersynchronization of epileptiform burst firing ; For generalized tonic-clonic seizures, partial seizures

Levetiracetam (TOPNOTCH)

not metabolized by CYP450 enzymes, eliminated in the kidneys in their unchanged form

Levetiracetam (TOPNOTCH)

multiple actions on synaptic function, probably via actions on phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic anhydrase)

Topiramate, Felbamate (TOPNOTCH)

also facilitate the inhibitory actions of GABA but its exact MOA is still unknown

Felbamate (TOPNOTCH)

Antiseizure drugs with the most number of MOA, undergo both hepatic and renal metabolism

Topiramate, Felbamate (TOPNOTCH)

Irreversibly inactivates GABA aminotransaminase (GABA-T) which terminates the action of GABA ; For GTC seizure

Vigabatrin (TOPNOTCH)

Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its reuptake, leading to prolongation of GABA effects ; For partial seizures

Tiagabine (TOPNOTCH)

SE: visual field defects

Vigabatrin (TOPNOTCH)

Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N receptors

Inhalational anesthetics (TOPNOTCH)

SE: megaloblastic anemia on prolonged exposure; Euphoria (laughing gas), bronchodilation

Nitrous Oxide (TOPNOTCH)

Lowest Potency (highest MAC) and least cardiotoxic

Nitrous Oxide (TOPNOTCH)

all inhaled anesthetcis cause bronchodilation except

Desflurane (TOPNOTCH)

SE: catecholamine-induced arrhythmias, peripheral vasodilation, bronchodilation

Isoflurane (TOPNOTCH)

SE: spike-and-wave activity in EEG, muscle twitching, breath-holding, myocardial depression, renal insufficiency (due to Flourine release), dec cardiac output, bronchodilation

Enflurane (TOPNOTCH)

has pungent odor which limits its use

Enflurane (TOPNOTCH)

SE: catecholamine-induced arrhythmias, myocardial depression, post-operative hepatitis, dec cardiac output, bronchodilation

Halothane (TOPNOTCH)

Highest potency and lowest MAC (very slow onset and recovery)

Methoxyflurane (TOPNOTCH)

a usual adjunct with inhalational anesthetics and IV opioids, has a slow onset but longer DOA

Midazolam (TOPNOTCH)

Blocks excitation by glutamate at NMDA receptors; For dissociative anesthesia (analgesia, amnesia and catatonia but with retained consciousness)

Ketamine (TOPNOTCH)

congener of Phencyclidine / angel dust

Ketamine (TOPNOTCH)

For general anesthesia to patients with limited cardiac or respiratory reserve

Etomidate (TOPNOTCH)

Interacts with mu, sigma, kappa receptors for endogenous opioid peptides ; For high risk patients who might not survive general anesthesia

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

SE: respiratory depression, chest wall rigidity (which may cause impaired ventilation) and constipation

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

Antidote is Naloxone / Naltrexone

Opioid toxicity (TOPNOTCH)

milk of anesthesia

Propofol, Fospropofol (TOPNOTCH)

Potentiates GABA-A receptors, blocks Na channels; For prolonged sedation esp in ICU patients and also in OPD surgeries

Propofol, Fospropofol (TOPNOTCH)

Blockade of Na channels slows which prevents axon potential propagation

Local Anesthetics (TOPNOTCH)

Shortest half-life among local anesthetics

Procaine (TOPNOTCH)

For local anesthesia, topical anesthesia

Benzocaine, Cocaine, Tetracaine (TOPNOTCH)

Use cautiously in sunburns, Topical only

Benzocaine (TOPNOTCH)

with intrinsic sympathomimetic activity so it does not need an alpha agonist (like epinephrine) to limit its systemic absorption

Cocaine (TOPNOTCH)

All local anesthetics are vasodilators EXCEPT

Cocaine (TOPNOTCH)

SE: light-headedness, sedation, restlessness, nystagmus, seizures, respiratory, CV depression, abuse liability, severe hypertension, cerebral hemorrhage, cardiac arrhythmia, MI

Cocaine (TOPNOTCH)

For local anesthesia, spinal anesthesia, epidural anesthesia, topical ophthalmic anesthesia

Tetracaine (TOPNOTCH)

Blockade of Na channels slows which prevents axon potential propagation; For local anesthesia, antiarrythmia (group 1B activity), used for post-MI and for digitalis toxicity

Lidocaine (TOPNOTCH)

For local anesthesia, dental anesthesia

Prilocaine (TOPNOTCH)

local anesthetic that can cause methemoglobinemia

Prilocaine (TOPNOTCH)

For local anesthesia, epidural anesthesia, intrathecal anesthesia

Bupivacaine (TOPNOTCH)

Use with caution in pregnant women and patients with cardiac disease (may cause heartblock, arrhyhtmia and hypotension)

Bupivacaine (TOPNOTCH)

Longest half-life among local anesthesia

Ropivacaine (TOPNOTCH)

Depolarizing Neuromuscular Blocker

Succinylcholine (TOPNOTCH)

Agonist at Ach-N receptors causing initial twitch then persistent depolarization

Succinylcholine (TOPNOTCH)

SE: muscle pain, hyperkalemia, increased intragastric pressure leading to regurgitation (aspiration), increased intraocular pressure, malignant hyperthermia

Succinylcholine (TOPNOTCH)

Metabolized by pseudocholinesterase ; may cause malignant hyperthermia if given together with inhaled anesthetics

Succinylcholine (TOPNOTCH)

a common SE for this group is Histamine release

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

Undergoes Hoffman elimination (rapid spontaneous breakdown)

Atracurium (TOPNOTCH)

converted to Laudanosine which can cause seizures

Atracurium (TOPNOTCH)

short-acting Non-Depolarizing Neuromuscular Blocker

Mivacurium (TOPNOTCH)

intermediate-acting Non-Depolarizing Neuromuscular Blocker ; Undergoes elimination in bile

Vecuronium (TOPNOTCH)

Suggamadex is a novel reversal agent for

Rocuronium (TOPNOTCH)

Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors; For skeletal muscle relaxation during intubation and general anesthesia

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

long-acting Non-Depolarizing Neuromuscular Blocker; may cause heart block

Pancuronium (TOPNOTCH)

Relatively contraindicated in myocardial ischemia; reverse effects with neostigmine

Tubocurarine (TOPNOTCH)

a dopamine precursor

Levodopa (TOPNOTCH)

inhibits peripheral metabolism via dopa decarboxylase

carbidopa (TOPNOTCH)

SE: GI upset (emesis), dyskinesia (choreoathetosis), behavioural changes (anxiety, agitation, confusion, delusion), on-off phenomena, wearing-off phenomena, postural hypotension, tachycardia

Levodopa-carbidopa (TOPNOTCH)

Partial agonist at dopamine D2 receptors in brain

Bromocriptine, Pergolide (TOPNOTCH)

For Parkinson's disease which is levodopa intolerance, hyperprolactinemia

Bromocriptine, Pergolide (TOPNOTCH)

SE: anorexia, n/v, dyskinesia, postural hypotension, behavioural changes, erythromelalgia, pulmonary infiltrate

Bromocriptine (TOPNOTCH)

Partial agonist at dopamine D3 receptors in brain

Pramipexole (TOPNOTCH)

SE: Contraindicated for patients with active peptic ulcer disease, psychotic illnesss or recent MI

Pramipexole, Ropinirole (TOPNOTCH)

Partial agonist at dopamine D3 receptors, antagonist at 5-HT and alpha adrenoceptors

Apomorphine (TOPNOTCH)

For off-periods of Parkinson's disease, alcoholism, opiate addiction, erectile dysfunction, alzheimer's disease

Apomorphine (TOPNOTCH)

Selective inhibitors of MAO type B leading to decreased degradation of dopamine, increases response to levodopa/carbidopa

Selegiline, Rasagiline (TOPNOTCH)

Block L-dopa metabolism by inhibiting catechol-O-methyltransferase in periphery and CNS, prolongs response to levodopa

Entacapone, Tolcapone (TOPNOTCH)

T or F: Entacapone only acts in the periphery while Tolcapone acts both in the periphery and CNS

TRUE (TOPNOTCH)

enhances dopaminergic transmission by unknown mechanism, maybe by influencing the synthesis, release or reuptake of dopamine

Amantadine (TOPNOTCH)

SE: behavioral changes (restlessness, agitation, insomnia, hallucination, psychosis), livedo reticularis, GI disturbances, urinary retention, postural hypotension, peripheral edema

Amantadine (TOPNOTCH)

Decrease the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

as adjunct for parkinson's disease and extrapyramidal symptoms caused by antipsychotics

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

Blocks D2 receptos more than 5-HT2 receptors

Typical Antipsyhotics (TOPNOTCH)

Typical Antipsychotic, SE: retinal deposits and arryhthmias

Thioridazine (TOPNOTCH)

has the Strongest autonomic effects; only antipsychotic with fatal overdose

Thioridazine (TOPNOTCH)

For schizophrenia and other psychotic disorders, huntington's disease and tourette's syndrome

Haloperidol, Droperidol (TOPNOTCH)

SE: extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, neuroleptic malignant syndrome

Haloperidol, Droperidol (TOPNOTCH)

Only antipsychotic that reduces the risk of suicide

Clozapine (TOPNOTCH)

For schizophrenia (refractory, suicidal) and other psychotic disorders

Clozapine (TOPNOTCH)

Blocks 5-HT2 receptors more than D2 receptors

Atypical Antipsychotics (TOPNOTCH)

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, hyperglycemia, hyperlipidemia, myocarditis, agranulocytosis, seizures, ileus, hypersalivation (sialotthea)

Clozapine (TOPNOTCH)

weight gain and hyperglycemia is prominent, safe in pregnancy

Olanzapine (TOPNOTCH)

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, somnolence, fatigue, sleep paralysis, hypnagogic hallucinations, cataracts, priapism, QT prolongation (TDP) ; safe in pregnancy

Quetiapine (TOPNOTCH)

Only antipsychotic approved for schizophrenia in the youth

Risperidone (TOPNOTCH)

Increased mortality in elderly patients with dementia-related psychosis ; can cause TDP

Ziprasidone (TOPNOTCH)

Least sedating atypical antipsychotics

Aripiprazole (TOPNOTCH)

Uncertain MOA but the proposed MOA is by inhibiting the enzyme involved in the recycling of neuronal membrane phosphoinositides which causes depletion of phosphatidylinositol bisphosphate, thus consequently decreasing IP3 and DAG leading to decreased neurotransmission

Lithium (TOPNOTCH)

SE: Tremor, sedation, ataxia, aphasia, thyroid enlargement, hypothyroidism, reversible nephrogenic diabetes insipidus, edema, acneiform skin eruption, leukocytosis, teratogen (ebstein's anomaly), bradycardia

Lithium (TOPNOTCH)

Block NE and 5-HT transporters leading to potentiation of NT action at postsynaptic receptors

Tricyclic Antidepressants (TOPNOTCH)

Tricyclic Antidepressants

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

For MDD (most effective), bipolar disorder, acute panic attacks, ADHD, chronic pain states, as sleeping aid, OCD ; this group is very useful for patients with psychomotor retardation, sleep disturbance, poor appetite and weight loss

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

3Cs of TCA overdose

Coma, Cardiotoxicity, Convulsions (TOPNOTCH)

longterm use may lead to down-regulation of Beta receptors leading to a decrease in BP and depression of cardiac conduction

Tricyclic Antidepressants (TOPNOTCH)

Inhibits neuronal reuptake of serotonin by inhibiting Serotonin Transporter (SERT)

SSRI (TOPNOTCH)

SSRIs

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

DOC for OCD, for MDD, anxiety, panic attacks, phobias, PTSD, GAD, bulimia, premenstrual dysphoric disorder, alcohol dependence

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

This antidepressant group can decrease appetite leading to weight loss

SSRI (TOPNOTCH)

Inhibits neuronal reuptake of serotonin and norepinephrine by binding to transporters for both 5HT and NE

SNRI (TOPNOTCH)

SNRIs

Venlafaxine, Duloxetine, Desvenlafaxine (TOPNOTCH)

differ from TCA in lacking blockade of H1, M and alpha receptors ; Increased risk for suicide in children and adolescents

SNRIs (TOPNOTCH)

Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT transporters

Serotonin antagonist (TOPNOTCH)

Antidepressant Serotonin antagonist

Trazodone, Nefazodone (TOPNOTCH)

Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor, blocks dopamine D2 receptors

Tetracyclics: Amoxapine (TOPNOTCH)

Increases amine release from nerve endings by antagonism of presynaptic a2 adrenoceptors, also blocks serotonin 5-HT2A receptors

Tetracyclics: Mirtazapine (TOPNOTCH)

Inhibits neuronal reuptake of dopamine and norepinephrine, increase dopamine and norepinephrine activity

Tetracyclics: Bupropion (TOPNOTCH)

Inhibits MAO type A and type B, increases CNS levels of NE and serotonin

Phenelzine, tranylcypromine (TOPNOTCH)

MAO-B selective inhibitor

Selegiline (TOPNOTCH)

Triad of opioid overdose

miosis, coma, respiratory depression (TOPNOTCH)

Strong agonist at u receptors; For severe pain, pain associated with acute MI, for pulmonary edema

Morphine (TOPNOTCH)

morphine is metabolized in the body to _____ which has equal analgesic activity as morphine

morphine-6-glucuronide (TOPNOTCH)

Strong agonist at u receptors; For severe pain, adjunct in anesthesia, chronic pain and breakthrough cancer pain

Fentanyl (TOPNOTCH)

Strong agonist at u and k receptors, inhibits pain neurotransmission, muscarinic blocking actions; For moderate to severe pain, labor analgesia, spasmodic pain (biliary, renal), preoperative sedation

Meperidine (TOPNOTCH)

Only opioid that does not cause miosis and biliary contraction

Meperidine (TOPNOTCH)

opioid of choice for pain relief in pancreatitis

Meperidine (TOPNOTCH)

metabolized to normeperidine which can cause _____ therefore contraindicated in patients with ______

seizure, seizure disorder (TOPNOTCH)

full opioid agonist, Strong agonist at u receptors, inhibits pain neurotransmission, binds NMDA receptors and antagonizes the effects of glutamate; For moderate to severe pain, opioid dependence, opioid withdrawal

Methadone (TOPNOTCH)

used as maintenance therapy for opioid dependence

Methadone (TOPNOTCH)

Decreases sensitivity of cough receptors, depressing the medullary cough center through sigma receptors stimulation; For cough suppression

Dextrometorphan, codeine (TOPNOTCH)

codeine is metabolized by CYP2D6 to ______

morphine (TOPNOTCH)

SE: miosis, restlessness, respiratory depression, increased ICP, postural hypotension, urinary retention, pruritus, addiction liability

Opioid analgesics (TOPNOTCH)

Mixed Agonist-Antagonist: Strong agonist at k receptors, weak antagonist activity at u receptors

Nalbuphine, buprenorphine, butorphanol, pentazocine (TOPNOTCH)

Weak agonist at u receptors, inhibits pain neurotransmission; For mild to moderate pain, restless leg syndrome

Propoxyphene, levopropoxyphene, dextropropoxyphene (TOPNOTCH)

Competitively blocks u, sigma and k receptors, rapidly reverses effects of opioid agonists; For opioid overdose, opioid and alcohol dependence

Naloxone, naltrexone, nalmefene (TOPNOTCH)

Weak agonist at u receptors, inhibits neuronal reuptake of serotonin and norepinephrine; For moderate pain, chronic pain syndrome, neuropathic pain

Tramadol (TOPNOTCH)

Required for the biosynthesis of heme and heme containing proteins, including hemoglobin and myoglobin; For Iron deficiency anmia, iron supplementation

Ferrous sulfate, Ferrous gluconate, Ferrous Fumarate, Iron dextran, Sodiun Ferric Gluconate complex, Iron sucrose (TOPNOTCH)

Chelates excess iron; For acute and chronic iron poisoning

Deferoxamine, Deferasirox (TOPNOTCH)

Cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methionine and metabolize methymalonyl-CoA; For vitamin B12 deficiency, megaloblastic anemia

Cyanocobalamin, Hydroxocobalamin (TOPNOTCH)

Precursor of an essential donor of methyl groups used for synthesis of amino acids, purines and deoxynucleotide; For Megaloblastic anemia, prevention of neutral tube defects(spina bifida), prevention of coronary artery disease

Folic acid (TOPNOTCH)

Agonist of erythropoietin receptors expressed by red cell progenitors; For Anemia, associated with chronic renal failure, cancer, HIV infection and prematurity

Epoetin Alfa, Darbepoetin alfa, Methoxy Polyethylene Glycol- Epoetin Beta (TOPNOTCH)

Binds receptors on myeloid progenitors and stimulates cell maturation and proliferation ; Accelerates neutrophil recovery and reduces incidence of infection; For neutrophenia associated with chemotheraphy, myelodysplasia, and aplastic anemia

(G-CSF) Filgrastim, Sargamostim (GM-CSF), Pegfilgrastim (TOPNOTCH)

Recombinant form of an endogenous cytokine; activates IL -11 receptors ; For secondary prevention of thrombocytopenia in patients undergoing chemotheraphy

Oprelvekin(IL-11),Thrombopoietin (TOPNOTCH)

nhibits rate-limit in enzyme in cholesterol biosynthesis (HMG-CoA reductase), Increased hepatic cholesterol uptake, Increased high affinity LDL receptors which leads to decreased LDL levels

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin, Cerivastatin (TOPNOTCH)

DOC for hypercholesterolemia(high LDL), decrease risk of acute coronary syndromes, ischemic stroke

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin, Cerivastatin (TOPNOTCH)

Prominent SE of statins: ____

Hepatoxicity, Myopathy, Rhabdomyolysis (TOPNOTCH)

Increased risk of myopathy and rhabdomyolysis when statins are used with

Fibrates (TOPNOTCH)

non-absorbable polyemers that bind bile acids and similar steroids in the intestines preventing their reabsorption, increases cholesterol utilization for replacement, modestly lowers LDL levels by increasing hepatic LDL receptors

Bile Acid Binding Resin (TOPNOTCH)

Bile Acid Binding Resin

Colesevelam, Colestipol, Cholestyramine (TOPNOTCH)

SE: Constipation, Bloating, Gritty taste, Gallstone formation, steatorrhea, malabsortion of fat soluble substances (vitamin k, folate)

Colesevelam, Colestipol, Cholestyramine (TOPNOTCH)

Selective inhibitor of the NCP1L1 transporter decreasing intestinal absorption of cholesterol and other phytosterols, decreases cholesterol hepatic pool, increases hepatic LDL receptors

NPC1L1 transporter inhibitor (TOPNOTCH)

NPC1L1 transporter inhibitor

Ezetimibe (TOPNOTCH)

Cholesterol analog, takes the place of dietary and billiary cholesterol, decreasing intestinal absorption of cholesterol and other phytosterols

Sitosterol (TOPNOTCH)

Decreases VLDL synthesis and LDL cholesterol concentrations, decreases hormone-sensitive lipase activity leading to decreased LDL levels, Increases HDL cholesterol by decreasing its catabolism

Niacin (TOPNOTCH)

DOC for increasing HDL levels

Niacin (TOPNOTCH)

SE: Flushing, nausea, vomiting, Pruritus, Acanthosis nigricans, Rashes, Gastrointestinal irritation, Hepatoxicity (mild), Hyperuricemia, Impaired glucose tolerance, Arrythmias, Amyblopia

Niacin (TOPNOTCH)

Activates PPAR-_ and increases expression of lipoprotein lipase and apolipoproteins (apoA-I, apoA-II) leading to enhanced clearance of TG-rich lipoproteins, Lowers triglycerides, Increases HDL

Fibrates (TOPNOTCH)

DOC for hypertriglyceridemia

Fibrates (TOPNOTCH)

Fibrates

Gemfibrozil, Fenofibrate, Bezafibrate (TOPNOTCH)

Fibrates have higher risk of gallstone formation if given together with ____

resins (TOPNOTCH)

Nonselective, irreversible COX 1&2 inhibitor. Reduces platelet production of thromboxane A2, temporarily inhibit Prostacyclin synthesis

Aspirin (TOPNOTCH)

Uncoupler of oxidative phosphorylation, associated with Reye syndrome in children

Aspirin (TOPNOTCH)

Reversbily inhibits the binding of fibrin and other ligands to the platelet GPIIb-IIIa receptor

GPIIb-IIIa inhibitor: Abciximab, Eptifibatide,Tirofiban (TOPNOTCH)

For prevention or arterial thrombosis (MI, TIA, CVD), Inflammatory disorders (rheumatic fever, juvenile rheumatoid arthritis, kawasaki disease)

Aspirin (TOPNOTCH)

Inhibits phosphodiesterase III and increases cAMP in platelets and blood vessels, Inhibits platelet aggregation and causes vasolidation

PDE III inhibitor: Dipyridamole, Cilostazol (TOPNOTCH)

additional MOA: inhibit uptake of adenosine by endothelial cells and RBC, thus increasing adenosine levels leading to inhibition of platelet aggregation

PDE III inhibitor: Dipyridamole, Cilostazol (TOPNOTCH)

Irreversibly inhibits binding of ADP to platelet receptors,thus reducing platelet aggregation

ADP inhibitor: Clopidogrel,Ticlopidine, Prasugel (TOPNOTCH)

Activates antithrombin III which Inactivates thrombin or factor IIa, factor IXa & factor Xa by forming stable complexes with them

Heparin (TOPNOTCH)

SE: Bleeding, transient Heparin-induced thrombocytopenia, Osteoporosis with chronic use

Heparin (TOPNOTCH)

DOC for anticoagulation during pregnancy ; administered IV or SC ; Monitor with aPTT,

Heparin (TOPNOTCH)

Antidote for heparin toxicity

Protamine Sulfate (TOPNOTCH)

Binds and potentiates effect of antithrombin III on factor Xa (more selective for Xa)

LMWH (TOPNOTCH)

LMWH

Enoxaparin, Dalteparin, Tinzaparin, Danaparoid, Fondaparinux (TOPNOTCH)

Does not require aPTT monitoring, Protamine sulfate is only partially effective in reversing effects

LMWH: Enoxaparin, Dalteparin, Tinzaparin, Danaparoid, Fondaparinux (TOPNOTCH)

Binds to thrombin's ative site and inhibits its enzymatic action

Direct Thrombin Inhibitors: Lepirudin, Desirudin, Bivalirudin, Argatroban, Dabigatran (TOPNOTCH)

bind to free and bound factor Xa

Direct Oral Factor Xa inhibitor: Rivaroxaban, Apixaban (TOPNOTCH)

Inhibits vitamin K epoxide reductase (responsible for y-carboxylation of the vitamin K- dependent clotting (factors II, VII, IX, X, Protein C & Protein S)

Warfarin (TOPNOTCH)

For chronic anticoagulation (DVT, atrial fibrillation, valve replacement)

Warfarin (TOPNOTCH)

SE: Bleeding, Teratogen (bone defects, hemorrhage), warfarin-induced skin necrosis (transient hypercoagulability)

Warfarin (TOPNOTCH)

Monitor effects with PT-INR

Warfarin (TOPNOTCH)

Antidote forwarfarin toxicity

Vitamin K or FFP (TOPNOTCH)

Chemical antagonist of heparin. Reverses excessive anticlotting activity of unfractionated heparin

Protamine Sulfate (TOPNOTCH)

Tissue plasminogen activator analog. Converts plasminogen to plasmin, which degrades the fibrin and fibrinogen, causing thrombolysis

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase (TOPNOTCH)

Tx should be done within 6 hrs, better if within 3hrs ; Antidote is AMINOCAPROIC ACID

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase (TOPNOTCH)

Competitively inhibits plasminogen activation thus inhibiting fibrinolysis

Tranexamic acid (TOPNOTCH)

For Vitamin K deficiency, Antidote to warfarin, prevention of hemorrhagic diatheses in newborns

Vitamin K1, K2 (Phytonadione, Menaquinone) (TOPNOTCH)

Vasopressin V2 receptor agonist, Increases factor VIII activity of patients with mild hemophilia A or VWD

Desmopressin (TOPNOTCH)

low doses undergo first order kinetics while high doses undergo zero order reaction ; Long term use reduces the risk of colon cancer

Aspirin (TOPNOTCH)

COX-2 > COX-1 inhibition

Meloxicam & Piroxicam (TOPNOTCH)

NSAIDs that can be used to close PDA

Ibuprofen and Indomethacin (TOPNOTCH)

has significant analgesic effect but not anti-inflammatory effect

Ketorolac (TOPNOTCH)

SE: Gastrointestinal toxicity, pancreatitis, Nephrotoxicity, Serious hematologic reactions, BM suppression

Indomethacin (TOPNOTCH)

Selective COX-2 inhibitor

Celecoxib, Etoricoxib, Parecoxib (TOPNOTCH)

Rofecoxib and Valdecoxib withdrawn due to

increased incidence of thrombosis (TOPNOTCH)

Selectively inhibits COX-3 in the CNS, Weak COX-1 and COX-2 inhibitor in the periphery, Inhibits prostaglandin synthesis

Paracetamol (Acetaminophen) (TOPNOTCH)

Inhibits AICAR transformylase and thymidylate snythetase, with secondary effects on polymorphonuclear chemotaxis

Methotrexate (TOPNOTCH)

DMARD of choice for Rheumatoid arthritis

Methotrexate (TOPNOTCH)

Rescue agent for Methotrexate toxicity

Leucovorin (Folinic acid) (TOPNOTCH)

Binds to TNF-a inhibitor

Infliximab, Adalimumab, Etanercept (TOPNOTCH)

SE: Bacterial infections (URTIs), reactivation of latent tuberculosis, lymphoma, Demyelination, Reactivation of Hepatitis B, Auto antibody formation (ANA, anti dsDNA), infusion reactions, hepatoxicity, hematotoxicity, cardiotoxicity

TNF-a inhibitor: Infliximab, Adalimumab, Etanercept (TOPNOTCH)

Antidote for paracetamol toxicity

N-acetyl cysteine (TOPNOTCH)

Forms 6-thioguanine, suppressing inosinic acid synthesis, B-cell and T-cell function, Immunoglobulin production and interleukin-2 secretion

Azathioprine (TOPNOTCH)

Cannot give _______ with azathioprine (the drug reduces xanthine oxide catabolism of purine analogs, increasing 6-thioguanine nucleotides, leading to serve leukopenia)

Allopurinol (TOPNOTCH)

Suppression of T-lymphocyte leading to decreased leukocyte chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA and RNA synthesis, trapping of free radicals

Chloroquine, Hydroxychloroquine (TOPNOTCH)

T or F: Chloroquine, Hydroxychloroquine are safe for pregnant patients

TRUE (TOPNOTCH)

Forms phospharamide mustard, which cross links DNA to prevent cell replication, Supresses T-cell and B-cell function

Cyclophosphamide (TOPNOTCH)

SE: hemorrhagic cystitis

Cyclophosphamide (TOPNOTCH)

Rescue agent for Cyclophosphamide toxicity

MESNA (TOPNOTCH)

Inhibits interleukin-1 and iterleukin-2 receptor production and secondarily inhibts macrophage-T-cell interaction and T-cell responsiveness

Cyclosporine (TOPNOTCH)

anti-IBD drug, active metabolite inhibits the release of inflammatory bowel cytokines

Sulfasalazine (TOPNOTCH)

Inhibits microtubule assembly and LTB4 production leading to decreased macrophage migration and phagocytosis

Microtubule assembly inhibtor: Colchicine (TOPNOTCH)

adverse effect which signals toxicity from colchicine

diarrhea (TOPNOTCH)

are weak acids that compete with uric acid for reabsorption in the PCT leading to increased uric acid excretion

Uricosuric agent: Probenecid, Sulfinpyrazone (TOPNOTCH)

may be given together with antimicrobial agents (particularly Pens) to prolong therapeutic effect by inhibiting renal tubular secretion of antibiotics

Probenecid (TOPNOTCH)

Active metabolite (alloxanthine) irreversibly inhibits xanthine oxidase and lowers production of uric acid

Xanthine oxidase inhibitor: Allopurinol, Febuxostat (TOPNOTCH)

1st line treatment of chronic gout, tumor lysis syndrome

Xanthine oxidase inhibitor: Allopurinol, Febuxostat (TOPNOTCH)

T or F: Allopurinol is more effective than Febuxostat

FALSE (TOPNOTCH)

Recombinant Growth hormone

Somatropin (TOPNOTCH)

Increases release of IGF-1 in the liver and carilage, stimulates skeletal muscle growth, amino acid transport, protein synthesis and cell proliferation

Somatropin (TOPNOTCH)

Recombinant IGF-1

Mecasermin (TOPNOTCH)

Somatostatin analog

Octreotide, Lanreotide (TOPNOTCH)

suppresses the release of growth hormones, glucagon, insulin, gastrin, IGF-1, serotonin and gastrointestinal peptides

Octreotide, Lanreotide (TOPNOTCH)

For Acromegaly, pituitary adenoma, carcinoid, gastrinoma, glucagonoma, variceal bleeding

Octreotide, Lanreotide (TOPNOTCH)

GH receptor antagonist ; For acromegaly

Pegvisomant (TOPNOTCH)

Gonadotropin analog (FSH analog) ; For Controlled ovarian hyperstimulation, infertility due to hypogonadism in men

Follitropin alfa, Follitropin beta, Urofollitropin (TOPNOTCH)

Gonadotropin analog (LH analog)

For Controlled ovarian hyperstimulation (ovulation induction), hypogonadotripic hypogonadism (TOPNOTCH)

SE: Headache, depression, edema, ovarian hyperstimulation syndrome, multiple pregnancies in women, gynecomastia in men

FHS and LH analogs (TOPNOTCH)

GnRH analog

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)

For Controlled ovarian hyperstimulation, endometriosis, myoma uteri, precocious puberty, postate CA

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)

there is exacerbation of symptoms in males with prostate CA and children with precocious puberty during the first few weeks of therapy

GnRH analog (TOPNOTCH)

For GnRH analogs: increased LH and FSH secretion with ________ administration , reduced LH and FSH secretion with ________ administration

intermittent ; prolonged continuous (TOPNOTCH)

GnRH antagonist

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

For Controlled ovarian hyperstimulation (prevents premature LH surge), advanced prostate CA

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

Does NOT cause tumor flare-up whe used for treatment of advanced prostate cancer

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

_____ is used for prostate CA while _____ prevent LH surge in controlled ovulation

Degarelix ; Ganirelix (TOPNOTCH)

Dopamine agonist, partial agonist at dopamine D2 receptors in brain ; For Hyperprolactinemia, Pituitary adenoma, acromegaly, Parkinson's disease

Bromocriptine, Carbegoline (TOPNOTCH)

Activates oxytocin receptors stimulates uterine contraction and labor, stimulates mammary glands, lactation and milk let-down

Oxytocin (TOPNOTCH)

For Labor induction, labor augmentation, control of uterine hemorrhage post-delivery

Oxytocin (TOPNOTCH)

oxytocin antagonist used in preterm labor

ATOSIBAN (TOPNOTCH)

ADH agonist, Vasopressin V2 receptor agonist

Desmopressin (TOPNOTCH)

For Central DI, Hemphilia A, von Willebrand's disease, Variceal bleeding, primary nocturnal seizures

Desmopressin (TOPNOTCH)

SE: Fetal distress, placental abruption, uterine rupture, fluid retention, hyponatremia, heart failure, seizures, hypotension

Oxytocin (TOPNOTCH)

ADH antagonist, Antagonist at V1a and V2 receptors

Conivaptan, Tolvaptan (TOPNOTCH)

_____ may occur with rapid correction of hyponatremia

Central pontine myelinolysis (TOPNOTCH)

Which is more selective for V2 receptors, Conivaptan or Tolvaptan?

tolvaptan (TOPNOTCH)

Thryoid hormone ; For Hypothyroidism, myxedema coma

Levothyroxine (T4), Liothyronine (T3) (TOPNOTCH)

T or F: Liothyronine has a faster onset but shorter half-life

TRUE (TOPNOTCH)

Inhibits thyroid peroxidase reactions, blocks iodine organification, inhibits peripheral conversion of T4 into T3

Propylthiouracil (PTU) (TOPNOTCH)

Drug of choice for pregnant hyperthyroid patients

Propylthiouracil (PTU) (TOPNOTCH)

Inhibits thyroid peroxidase reactions, blocks iodine organification

Methimazole, Carbimazole (TOPNOTCH)

Inhibit iodine organification and hormone release leading to reduced size and vascularity of thyroid gland

Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)

onset is more rapid (2-7 days) but effect is transient ; Should not be used alone (escape in 2-8 weeks); prevents radiation induced thryoid damage; prenatal exposure causes fetal goiter

Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)

Beta blocker control HR and other cardiac abnormalities of severe thyrotoxicosis, slows pacemaker activity; inhibits peripheral conversion of T4 into T3

Propranolol, Esmolol, Metoprolol, Atenolol (TOPNOTCH)

_____ may be used to treat thyrotoxicosis-related arrhythmias

Esmolol (TOPNOTCH)

Iodide, emits beta rays causing destruction of thyroid parenchyma

Radioactive Iodine (TOPNOTCH)

For hyperthyroidism, permanent cure of thyrotoxicosis without surgery and no effect on other tissues

Radioactive Iodine (TOPNOTCH)

Preferred treatment for most patients due to ease of administration, effectiveness, low expense and absence of pain; contraindicated in pregnant women or nursing mothers

Radioactive Iodine (TOPNOTCH)

Low Potency Glucocorticoid (GC)

Desonide (TOPNOTCH)

Medium Potency GC

Fluticasone, Mometasone (TOPNOTCH)

High Potency GC

Desoximetasone, Clobetasol (TOPNOTCH)

Effects: stimulate gluconeogenesis, increased fat deposition, protein catabolism, inhibit cell-mediated immunologic functions, lymphotoxic, increased neutrophils, decreased lymphocytes, eosinpphils, basophils and monocytes, inhibit leukocyte migration, inhibit PLA2

Glucocorticoids (TOPNOTCH)

_____ is the active metabolite of prednisone

prednisolone (TOPNOTCH)

SE: Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes (psychosis)

Glucocorticoids (TOPNOTCH)

For supressession of inflammation and immune response, hematopoeitic cancers, transplant rejection, collagen and rheumatic disease, lung maturation in preterm labor

Glucocorticoids (TOPNOTCH)

strong agonist of mineralocorticoid receptors and moderate activation of glucorticoid receptors

Mineralocorticoid (TOPNOTCH)

Increases Na reabsorption, K and H excretion ; For Chronic adrenal insufficiency (Addison's disease), Congenital adrenal hyperplasia, adrenal replacement therapy post-adrenalectomy

Mineralocorticoid (TOPNOTCH)

Mineralocorticoid

Fludrocortisone, Deoxycorticosterone (TOPNOTCH)

Additive hypokalemia with loop diurectics and thiazides

Fludrocortisone, Deoxycorticosterone (TOPNOTCH)

Glucorticoid synthesis inhibitor, inhibits desmolase activity, blocking conversion of cholesterol to pregnenolone

Aminoglutethimide (TOPNOTCH)

Glucorticoid synthesis inhibitor, inhibits cholesterol side chain cleavage, cytochrome P450 enzymes and other enzymes necessary for synthesis of all steroids

Ketoconazole (TOPNOTCH)

Ketoconazole is CYP450 inhibitor or inducer?

Inhibitor (TOPNOTCH)

Glucorticoid synthesis inhibitor, selective inhibitor of steroid-11 hydroxylation

Metyrapone (TOPNOTCH)

DOC for pregnant patients with Cushing's syndrome

Metyrapone (TOPNOTCH)

competitive inhibitor at the GC receptor as well as progesterone receptor ; For Cushing's syndrome

Mifepristone (RU486) (TOPNOTCH)

also used as an approved abortifacient for medical abortion (usually together with misoprostol)

Mifepristone (RU486) (TOPNOTCH)

Activates etrogen receptors, leads to changes in rates of trasncription of estrogen-regulated genes

Estrogens: Ethinyl Estradiol, Mestranol, Estradiol cypionate, Premarin (TOPNOTCH)

Synthetic estrogen (nonsteroid); activates estrogen receptors; leads to changes in rates of transcription of estrogen-regulated genes ; For Atrophic vaginitis, hormone replacement therapy, prevention of adverse pregnancy outcomes, metastatic prostate CA

Diethylstilbestrol (TOPNOTCH)

associated with Infertility, ectopic pregnancy, clear cell vaginal adenocarcinoma in daughters of women who used this drug

Diethylstilbestrol (TOPNOTCH)

activates progesterone receptors, change rates of transcription of progesterone-regulated genes ; For Hormone replacement therapy, contraception, assisted reproduction, anovulation induction

Progestins: Norgestrel, Medroxyprogesterone, Norethindrone, Norgestimate, Desogestrel,Megestrol (TOPNOTCH)

IM depot preparation

Medroxyprogesterone Acetate (TOPNOTCH)

Must be taken within 72 hours of unprotected sexual intercourse

Levonorgestrel (TOPNOTCH)

Estrogen antagonist actions in breast tissue and CNS, Estrogen agonist effects in uterus, liver and bone

Tamoxifen, Torimefene (TOPNOTCH)

Estrogen antagonist actions in breast tissue, uterus, and CNS, Estrogen agonist effects in liver and bone

Raloxifene (TOPNOTCH)

Partial agonist in pituitary, reduces negative feedback by estradiol, increases FSH and LH output, For Induction of ovulation

Clomiphene (TOPNOTCH)

Reduces estrogen synthesisby inhibiting aromatase ; For breast CA, precocious puberty

Anastrozole, Letrozole, Exemestane (TOPNOTCH)

Ovarian inhibitor, weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors ; For Endometriosis, Fibrocystic disease, Hemophilia, Angioneurotic edema

Danazol (TOPNOTCH)

Activates androgen receptors, promotes development of male characteristics, increases body muscle bulk and RBC production

Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)

Effects: induces secretory changes in the endometrium, stabilize the endometrium, affect carbohydrate metabolism and stimulate deposition of fat, high doses suppress FSH and LH secretion

progesterone (TOPNOTCH)

Effects: secondary sexual characteristics, fertility and libido, male pattern baldness, increases muscle mass, increased RBC production, decreased urea nitrogen excretion

Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)

anabolic steroids

Oxandrolone, Stanozolol, Nandrolone (TOPNOTCH)

Competitive antagonist at androgen receptor ; For Prostate CA, surgical castration

Flutamide, Bicalutamide, Nilutamide (TOPNOTCH)

Antagonist at androgen receptor. Marked progestational effect that suppresses the feedback enhancement of LH and FSH

Cyproterone (TOPNOTCH)

Androgen synthesis inhibitor, inhibits 5a reducase enzyme that converts testosterone to dihydrotestosterone ; For BPH, Male pattern baldness. Hirsutism

Finasteride, Dutasteride (TOPNOTCH)

Activates a Tyrosine Kinase typer of receptorsleading to a reducting of circulating glucose: promotes glucose transport and oxidation; glycogen, lipid, protein synthesis and regulation of gene expression

Insulin (TOPNOTCH)

Rapid Acting Insulin

Lispro, Aspart, Glulisine (TOPNOTCH)

Short Acting Insulin

Regular Insulin (TOPNOTCH)

Intermediate Acting Insulin

NPH, Lente (TOPNOTCH)

Long Acting Insulin

Detemir, Glargine, Ultralente, Lantus (TOPNOTCH)

peakless insulins

Long Acting Insulin (TOPNOTCH)

acts as an insulin secretagogue, increases insulin secretion from pancreatic beta cells by closing ATP sensitive K+ channels leading to depolarization of the B cell

Sulfonylureas (TOPNOTCH)

2nd generation sulfonylurea

Glipizide, Glibenclamide, Glimepiride, Gliclazide, Glyburide (TOPNOTCH)

1st generation sulfonylurea

Tolazamide, Tolbutamide, Chlorpropamide (TOPNOTCH)

T or F: 1st gen SUs have less hypoglycemia than 2nd gen

FALSE (TOPNOTCH)

Insulin Secretagogue, similar to sulfonylureas with some overlap in binding sites, reduces circulating glucose, increases glycogen, fat and protein formation and gene regulation

Meglitinides (TOPNOTCH)

Meglitinides

Repaglinide, Nateglinide (TOPNOTCH)

Least hypoglycemia among OHAs

Meglitinides (TOPNOTCH)

Reduced hepatic and renal gluconeogenesis with decreased endogenous glucose production, activates AMP-stimulated protein kinase leading to inhibition of gluconeogenesis

Biguanides (TOPNOTCH)

Biguanides

Metformin (TOPNOTCH)

DOC for obese diabetics

Metformin (TOPNOTCH)

Inhibits intestinal alpha-glucosidases , reduces conversion of starch and disacchardies to monosaccharidea, reduces post prandial hyperglycemia

Alpha Glucosidase Inhibitors (TOPNOTCH)

Alpha Glucosidase Inhibitors

Acarbose, Miglitol (TOPNOTCH)

Regulates gene expression by binding to PPAR-gamma and PPAR-alpha which increases tissue sensitivity, increases glucose uptake in muscle and adipose tissue, inhibits hepatic gluconeogenesis, effects on lipid metabolism and distribution of body fat, control of fasting and postprandial glucose, decreased risk of DM in high-risk patients

Thiazolidinediones (TOPNOTCH)

Thiazolidinediones

Pioglitazone, Rosiglitazone (TOPNOTCH)

binds to PPAR-gamma and PPAR-alpha

Pioglitazone (TOPNOTCH)

binds to PPAR-gamma ONLY

Rosiglitazone (TOPNOTCH)

SE: Fluid retention, weight gain, congestive heart failure, fractures esp in women, cardiovascular events, hepatotoxicity, macular edema, dyslipidemia, increased risk of MI

Thiazolidinediones (TOPNOTCH)

Analog of GLP-1, Binds to GLP-1 receptors which leads to reducetion of post-meal glucose excursions, increases glucose-mediated insulin release, lowers glucagon levels, slows gastric emptying time, produces satiety

Exenatide (TOPNOTCH)

Dipeptidyl Peptidase-4 Inhibitors, blocks degradation of GLP-1, raises circulating GLP-1 levels, reduces post-meal glucose excursions, increases glucose mediated insulin release, lowers glucagon levels, slows gastric emptying time, decreases appetite

Sitagliptin, Linagliptin (TOPNOTCH)

Analog of amylin, Binds to amylin receptors, reduce post-meal glucose excursions, lowers glucagon levels, slows gastric emptying, decreases appetite

Pramlintide (TOPNOTCH)

Bile acid binder, lowers glucose through unknown mechanisms

Colesevelam hydrochloride (TOPNOTCH)

INACTIVE Vitamin D

Cholecalciferol, Ergocalciferol (TOPNOTCH)

ACTIVE Vitamin D

Calcitriol, Doxercalciferol, Paricalcitol, Calcipotriene (TOPNOTCH)

Suppress the activity of osteoclasts in part via inhibition of farnesyl pyrophosphate synthesis, inhibit resorption and formation of bone by acting on the basic hydroxyapatite crystal structure

Bisphosphonates (TOPNOTCH)

Bisphosphonates

Alendronate, Risedronate, Ibandronate, Pamidronate, Zoledronate, Etidronate, Tiludronate, Zoledronic acid (TOPNOTCH)

Recombinant PTH, Acts via cognate G protein coupled receptors, stimulates bone formation when given in low intermittent doses

Teriparatide (TOPNOTCH)

Acts via cognate G protein coupled receptors; suppresses bone resorption ; For Paget's disease of the bone, hypercalcemia, osteoporosis, tumor marker for thyroid CA

Calcitonin (TOPNOTCH)

Interacts selectively with estrogen receptors, inhibits PTH-stimulated bone resorption without stimulating breast or endometrial hyperplasia, delay bone loss in post-menopausal women

Raloxifene (TOPNOTCH)

Monoclonal antibody, binds to RANKL and prevents it from stimulating osteoclast differentiation and function, blocks bone resorption

Denosumab (TOPNOTCH)

Activates the calcium sensing receptors in the parathyroid gland, inhibits PTH secretion

Calcium Receptor Antagonist: Cinacalcet (TOPNOTCH)

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls

Penicillin, Cephalosporins (TOPNOTCH)

DOC for syphillis, for streptococcal, meningococcal, G+ bacilli, spirochete infection

Natural Penicillins: Penicillin G, Penicillin V (narrow spectrum penicillin) (TOPNOTCH)

For staphylococcal infections

Anti-Staphylococcal Penicillins: Methicillin, nafcillin, oxacillin, cloxacillin (very narrow spectrum) (TOPNOTCH)

all penicillins are excreted unchanged in the urine EXCEPT for _____which is excreted in the bile

Nafcillin (TOPNOTCH)

Pens For enterococci, Listeria, E. coli, Proteus, H. influenza, Moraxella

Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)

Pens For Pseudomonas, Enterobacter, Klebsiella

Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)

all Cephs have renal excretion EXCEPT ______

Cefoperazone and Ceftriaxone (TOPNOTCH)

Cephs for For surgical prophylaxis, bone infections, infections due to staph and strep, E. coli, Klebsiella, G+ cocci

First Generation Cephs (TOPNOTCH)

Increases nephrotoxicity of aminoglycosides

Cephs (TOPNOTCH)

For surgical prophylaxis, bone infections, infections due to staph strep and E. coli, Enterobacter, Neisseria, infections against anaerobes (Bacteroides), sinus ear and respiratory infections by Klebsiella andHemophilus

Second Generation Cephs (TOPNOTCH)

Second Generation Cephs

Cefamandole, cefaclor, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin, cefmetazole, cefotetan (TOPNOTCH)

First Generation Cephs

Cefazolin, cefadroxil, cephalothin, cephapirin, cephradine, cephalexin (TOPNOTCH)

Cephs with slight less activity against G+ but extended G- activity

Second Generation Cephs (TOPNOTCH)

decreased gram + coverage, increased gram - activity (pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, Haemophilus ; DOC for gonorrhea

Third Generation Cephs (TOPNOTCH)

DOC for gonorrhea

Ceftriaxone and Cefixime (TOPNOTCH)

Third Generation Cephs

Cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, ceftibuten (TOPNOTCH)

all can Third gen Cephs can penetrate the BBB EXCEPT _____

Cefoperazone and Cefixime (TOPNOTCH)

More resistant to beta-lactamase produced by Enterobacter, Haemophilus, Neisseria and Pneumococcal

Fourth Generation Cephs (TOPNOTCH)

Fourth Generation Cephs

Cefipime (TOPNOTCH)

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls, wide coverage against gram + gram - bacteria and anaerobes ; For infections resistant to other antibiotics EXCEPT MRSA, DOC for Enterobacter, Citrobacter and Serratia

Carbapenems (TOPNOTCH)

Carbapenems

Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)

Imipenem given with Cilastatin which acts as ______

Dehydropeptidase enzyme inhibitor (TOPNOTCH)

Monobactam

Aztreonam (TOPNOTCH)

Resistant to beta-lactamase, no activity against gram + bacteria or anaerobes

Aztreonam (TOPNOTCH)

No cross-allergenicity with Pens

Aztreonam (TOPNOTCH)

Inhibits inactivation of penicillins by bacterial beta-lactamase (penicillinase)

Beta-Lactamase Inhibitors (TOPNOTCH)

Beta-Lactamase Inhibitors

Clavulanic acid , sulbactam, tazobactam (TOPNOTCH)

Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan --> inhibit transglycosylation --> prevent elongation and cross-linking of peptidoglycan chain

Glycopeptides: Vancomycin, teicoplanin, telavancin (TOPNOTCH)

For MRSA, PRSP, as alternative for pseudomembranous colitis

Vancomycin (TOPNOTCH)

SE: red man syndrome, nephrotoxicity, ototoxicity, chills, fever, phlebitis

Vancomycin (TOPNOTCH)

Interferes with a late stage in cell wall synthesis in gram + organisms ; For gram + bacteria

Bacitracin (TOPNOTCH)

Reserved for topical use only due to marked nephrotoxicity

Bacitracin (TOPNOTCH)

Blocks incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan ; For drug-resistant TB

Cycloserine (TOPNOTCH)

inhibits cytosolic enolpyruvate transferase --> prevents formation of N-acetylmuramic acid

Fosfomycin (TOPNOTCH)

same spectrum of activity as Vancomycin ; For VRE, VRSA, for G+ activity, against endocarditis and sepsis

Daptomycin (TOPNOTCH)

Inhibits transpeptidation (catalyzed by peptidyl transferase) by blocking the binding of aminoacyl moiety of the charged tRNA to the acceptor site o mRNA at 50S subunit, basteriostatic

Chloramphenicol (TOPNOTCH)

For meningitis (Strep pneumonia, H influenza, Neisseria meningitides), back up for Salmonella, Rickettsia, Bacteroides, Wide spectrum antibiotic

Chloramphenicol (TOPNOTCH)

Binds 30s ribosomal subunit thus preveting the binding of tRNA to mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ and G-), anaerobes and atypicals

Tetracyclines (TOPNOTCH)

_____ has the broadest spectrum of all tetracyclines and has the longest t1/2 (30-36hrs)

Tigecycline (TOPNOTCH)

SE: GI disturbances (enetrocolitis, nausea, diarrhea, vomiting), teratogen (tooth enamel dysplasia/discoloration), hepatotoxicity, nephrotoxicity, photosensitivity n(esp. demeclocycline), vestibulotoxicity, candidiasis, bacterial superinfection with S. aureus and C. difficile, Fanconi syndrome

Tetracyclines (TOPNOTCH)

Tetracyclines

Tetracycline, doxycycline, minocycline, tigecycline, demeclocycline (TOPNOTCH)

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For community-acquired pneumonia, pertussis, diphtheria, chlamydial infections

Macrolides (TOPNOTCH)

Macrolides

Erythromycin, azithromycin, clarithromycin, telithromycin (TOPNOTCH)

______ is used as an alternative Ceftriaxone in Gonorrhea and to Pen G in syphilis

Azithromycin (TOPNOTCH)

______ is used for macrolide-resistance

telithromycin (TOPNOTCH)

a narrow spectrum macrolide, for G+ and anaerobe, low oral bioavailability

Fidaxomicin (TOPNOTCH)

as effective as Vancomycin as treatment for C. difficile possibly with lower relapse rate

Fidaxomicin (TOPNOTCH)

GI disturbance, skin rash, neutropenia, hepatic dysfunction, possible superinfection (Pseudomembranous colitis - C. difficile overgrowth)

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For anaerobic infections (Bacteroides), alternative against gram + cocci (MRSA), endocarditis prophylaxis esp in those allergic to Pens, PCP pneumonia, toxoplasmosis (+ Pyrimethamine), skin and soft tissue infection

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

Binds 50s ribosomal subunit, constricting the channel where polypeptides are extruded thus tRNA synthetase is also inhibited --> decreased free tRNA

Streptogramin: Quinupristin-Dalfopristin (TOPNOTCH)

Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation by blockin formation of the tRNA-ribosome-mRNA ternary complex, bacteriostatic ; Reserved for infections caused by drug-resistant gram + cocci (MRSA, VRE, PRSP), Listeria, Corynebacteria

Oxazolidinone: Linezolid (TOPNOTCH)

For serious infections caused by aerobic gram _ bacteria (E.coli, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas, Serratia, Haemophilus, Moraxella, Shigella), endocarditis, ocular infections

Aminoglycosides (TOPNOTCH)

Least resistance and narrowest therapeutic window ; used for streptomycin-resistant TB

Amikacin (TOPNOTCH)

For TB, tularaemia, bubonic plague, brucellosis

Streptomycin (TOPNOTCH)

SE: nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade

Aminoglycosides in general (TOPNOTCH)

SE: hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade, teratogen (congenital deafness), injection site reactions

Streptomycin (TOPNOTCH)

_____ is most ototoxic of all Aminoglycosides (AG) while _____ has the most skin reactions

kanamycin ; Neomycin (TOPNOTCH)

For drug-resistant gonorrhoea, gonorrhoea in penicillin allergic patients

Spectinomycin (TOPNOTCH)

For Treatment of serious infections caused by organisms resistant to other aminoglycosides

Netilmicin (TOPNOTCH)

Inhibits dihydropteroate synthase, bacteriostatic

Sulfonamides (TOPNOTCH)

low solubility in acidic urine causing formation of stones

Sulfonamides (TOPNOTCH)

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase , bactericidal

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

SE: GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, hypersensitivity, hematotoxicity, kernicterus ; antifolate effects (megaloblastic anemia, leukopenia, granulocytopenia)

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV (G+) and Topoisomerase II (G-)

Fluoroquinolones (TOPNOTCH)

For infections of the urogenital and GI tract by G- (gonococci, E. coli, Klebsiela, Campylobacter, Enterobacter, Pseudomonas, Salmonella, Shigella), respiratory tract, skin and soft tissue infection

Fluoroquinolones (TOPNOTCH)

CI in pregnancy and in children (damage growing cartilage --> arthropathy)

Fluoroquinolones (TOPNOTCH)

GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, phototoxicity, CNS effects (dizziness, headache), tendinitis and tendon rupture, opportunistic infection by Candida and Streptococci

Fluoroquinolones (TOPNOTCH)

Second Generation Fluoroquinolones

Ciprofloxacin, ofloxacin (TOPNOTCH)

First Generation Fluoroquinolones

Norfloxacin, Nalidixic acid (TOPNOTCH)

Third Generation Fluoroquinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

Respiratory Quinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

newest members of the Fluoroquinolone family and are condisered to have the broadest spectrum of activity with increased activity aginst anaerobes ang atypical agents

Moxifloxacin and Gemifloxacin (TOPNOTCH)

Fourth Generation Fluoroquinolones

Trovafloxacin, Gatifloxacin (TOPNOTCH)

FQ elimination is via kidneys by tubular secretion (may compete with probenecid for excretion) EXCEPT

Moxifloxacin (TOPNOTCH)

additional SE of which FQs: diabetes, hepatotoxicity

diabetes (gatifloxacin), hepatotoxicity (trovafloxacin) (TOPNOTCH)

Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain, bactericidal

Metronidazole, tinidazole (TOPNOTCH)

For anaerobic or mixed intra-abdominal infections, vaginitis (trichomonas, gardnerella), pseudomembranous colitis, brain abscess, protozoal infections

Metronidazole, tinidazole (TOPNOTCH)

DOC for amoebiasis, giardiasis and Pseudomembranous colitis

Metronidazole (TOPNOTCH)

single OD dose can prevent recurrent UTI

Nitrofurantoin (TOPNOTCH)

SE: GI irritation, metallic taste, headache, dark urine, leukopenia, dizziness, ataxia, neuropathy, seizures and disulfiram reaction

Metronidazole (TOPNOTCH)

acidification of urine enhances activity ; adjust dose in renal patients

Nitrofurantoin (TOPNOTCH)

Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase, bactericidal ; For UTI (except Proteus and Pseudomonas)

Nitrofurantoin (TOPNOTCH)

Inhibits mycolic acid synthesis, bactericidal

Isoniazid (TOPNOTCH)

SE: hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, insomnia, restlessness, muscle twitching), acute hemolysis in G6PD deficiency, drug-induced lupus

Isoniazid (TOPNOTCH)

Most impt drug in TB

Isoniazid (TOPNOTCH)

prevent neurotoxicity of Isoniazid by giving

pyridoxine (vit B6) (TOPNOTCH)

given as a sole drug for prophylaxis of close contacts of TB Px and skin test converters

Isoniazid (TOPNOTCH)

Inhibits DNA-dependent RNA polymerase, bactericidal

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

red-orange urine, light chain proteinuria, skin rash, thrombocytopenia, nephritis, hepatotoxicity, flulike syndrome, anemia, impair antibody response

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

CYP450 inhibitor: Rifampicin or INH

INH (TOPNOTCH)

CYP450 inducer: Rifampicin or INH

Rifampicin (TOPNOTCH)

Inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall, bacteriostatic

Ethambutol (TOPNOTCH)

SE: dose-dependent visual disturbances (decreased visual acuity, red green color blindness, retrobulbar neuritis, retinal damage, optic neuritis), headache, confusion, hyperuricemia, peripheral neuritis

Ethambutol (TOPNOTCH)

Unknow MOA, bacteriostatic but can be bactericidal on actively dividing mycobacteria, is metabolized to pyrazinoic acid, t 1/2 is increased in liver and kidney disease

Pyrazinamide (TOPNOTCH)

SE: hepatotoxicity, nongouty polyarhtralgia, asymptomatic hyperuricemia, myalgia, GIT irritation, maculopapular rash, porphyria, photosensitivity ; CI in pregnancy

Pyrazinamide (TOPNOTCH)

Most hepatotoxic anti-TB drug

Pyrazinamide (TOPNOTCH)

Most active drug against M. leprae

Dapsone (TOPNOTCH)

_______ is a repository form of dapsone which has drug action that can last for several months

Acedapsone (TOPNOTCH)

Binds to guanine bases in bacterial DNA, bactericidal ; For leprosy

Clofazimine (TOPNOTCH)

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

Amphotericin B (TOPNOTCH)

WIDEST antifungal spectrum

Amphotericin B (TOPNOTCH)

For systemic fungal infections (aspergillus, blastomyces, candida, Cryptococcus, histoplasma, mucor), for initial induction before followup treatment with azoles, can be used topically in mycotic corneal ulcers and keratitis

Amphotericin B (TOPNOTCH)

Accumulated in fungal cells by the action of permease and converted by cytosine deaminase to 5-FU, which inhibits thimidylate synthase, pyrimidine antimetabolite, fungistatic

Flucytosine (TOPNOTCH)

SE: infusion reactions (chills, fever, muscle spasms, vomiting, hypotension), dose limiting nephrotoxicity (decreased GFR, ATN with magnesium and potassium wasting, decreased erythropoietin), neurotoxicity (seizure, neuronal damage)

Amphotericin B (TOPNOTCH)

Inhibit 14-demethylase --> decreased ergosterol production --> increased permeability of cell membrane, Inhibits fungal P450-dependent enzymes blocking ergosterol synthesis, fungistatic

Ketoconazole (TOPNOTCH)

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, drug interaction, gynecomastia, menstrual irregularities and infertility

Ketoconazole (TOPNOTCH)

DOC for candidiasis (esophageal, oropharyngeal, vulvovaginitis), coccidioidomycosis, cryptococcal meningitis (treatment and prophylaxis)

Fluconazole (TOPNOTCH)

alternative to Ampho B in the treatment of C. neoformans, as effective as Ampho B in candidemia

Fluconazole (TOPNOTCH)

DOC for blastomycosis, sporotrichosis, dermatophytosis esp onchomycosis, chromoblastomycosis ; alternative for infections due to Aspergillus, Coccidioides, Cryptococcus and Histoplasma , for esophageal candidiasis resistant to fluconazole

Itraconazole (TOPNOTCH)

co-DOC for invasive aspergillosis, alternative in candidemia, for fluconazole-resistant organisms, for candidal esophagitis and stomatitis in AIDS patients

Voriconazole (TOPNOTCH)

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, blurring of vision in 30% of patients, CI in pregnancy

Voriconazole (TOPNOTCH)

as salvage therapy in invasive aspergillosis

Posaconazole (TOPNOTCH)

BROADEST spectrum triazole ; the only azole with activity against Rhizopus sp. (mucormycosis

Posaconazole (TOPNOTCH)

azoles that are limited to topical use because of systemic toxicity

Clotrimazole, miconazole, ketoconazole (TOPNOTCH)

Inhibit beta-glucan synthase which produces (1-->2) glycan which is a cell wall component, thus decreasing fungal cell wall synthesis, fungostatic

Echinocandins: Caspofungin, anidulafungin, micafungin (TOPNOTCH)

Interferes with microtubule function in dermatophytes, inhibits synthesis and polymerization of nucleic acids, fungistatic

Griseofulvin (TOPNOTCH)

Inhibits with ergosterol synthesis by inhibiting fungal squalene oxidase leading to increased squalene which interferes with ergosterol synthesis, fungicidal

Terbinafine (TOPNOTCH)

absorption is increased by intake of fatty meal

Griseofulvin (TOPNOTCH)

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

Nystatin (TOPNOTCH)

For candidiasis ((oropharyngeal, esophageal and vaginal), for GI fungal infections in patients with impaired defense mechanisms

Nystatin (TOPNOTCH)

Activated by viral thymidine kinase (TK) to forms that inhibit viral DNA polymerase, guanosine analog, competitive substrate for DNA polymerase, causes chain termination after its incorporation into the viral DNA

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

For infections due to HSV1, HSV2, VZV (mucocutaneous and genital herpes, prophylaxis in AIDS and in other Immunocompromised states such as organ transplant patients, herpes encephalitis, neonatal HSV infection etc.

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

_____ is a prodrug that is converted to Acyclovir and reached plams levels 3-5x (longer t1/2) more than acyclovir

Valacyclovir (TOPNOTCH)

____ is a prodrug which is converted to Penciclovir in vivo

Famciclovir (TOPNOTCH)

Inhibits fusion between the HSV envelope and plasma membrane, prevents viral entry and subsequent replication

Docosanol (TOPNOTCH)

Inhibits viral DNA polymerase causing chain termination, guanosine derivative

Ganciclovir, valganciclovir (TOPNOTCH)

For infections due to CMV, HSV1, HSV2, VZV ; For prohylaxis and treatment of CMV retinitis and other CMV infections in the immunocompromised patients

Ganciclovir, valganciclovir (TOPNOTCH)

Inhibits viral DNA polymerase causing chain termination ; For CMV retinitis, mucocutaneous HSV infections, acyclovir-resistance, ganciclovir-resistance, genital warts and molluscum contangiosum

Cifodovir (TOPNOTCH)

Inhibits viral RNA polymerase, DNA polymerase, and HIV reverse transcriptase, binds to pyrophosphate binding site

Foscarnet (TOPNOTCH)

adenine analog ; For HSV, VZV, CMV

Vidarabine (TOPNOTCH)

pyrimidine analogs ; For herpes keratitis (HSV-1)

Idoxuridine, trifluridine (TOPNOTCH)

antisense oligonucleotide that binds to mRNA of CMV causing inhibition of early protein synthesis ; For CMV retinitis

Fomivirsen (TOPNOTCH)

Inhibit HIV reverse transcriptase after phosphorylation by cellular enzymes, acts as chain terminators via insertion into the growing DNA chain

NRTI (TOPNOTCH)

NRTIs

Abacavir, Didanosine (ddI), Emtricitabine, Lamivudine (3TC), Stavudine (d4T), Tenofovir, Zalcitabine (ddC),Zidovudine (ZDV) (TOPNOTCH)

Inhibits HIV reverse transcriptase, no phosphorylation required, do not compete with nucleoside triphosphate

NNRTI (TOPNOTCH)

NNRTIs

Delavirdine, efavirenz, etravirine, nevirapine (TOPNOTCH)

cleaves precursor polyprotein to form the final structural protein of the mature virion core, inhibits viral protein processing

Protease Inhibitor (TOPNOTCH)

Protease Inhibitor

Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir-Ritonavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir (TOPNOTCH)

Binds to gp41 subunit of viral envelope glycoprotein, preventing fusion of viral and cellular membranes

Fusion Inhibitor: Enfuvirtide (TOPNOTCH)

Blocks viral attachment by blocking CCR5, a transmembrane protein involved in the attachment of HIV to host cell

CCR5 receptor antagonist: Maraviroc (TOPNOTCH)

Inhibit early step replication and prevent uncoating by binding to M2 proton channels ; For influenza A and rubella

Uncoating inhibitors: Amantadine, rimantadine (TOPNOTCH)

Inhibits neuraminidase which cleaves sialic acid residues from viral proteins and surface proteins of infected cells , decrease release of progeny virus

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

DOC for influenza (including H1N1)

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

cytokine, increased activity of JAKS leading to phosphorylation of signal transducers and activation of transcription (STATS) which causes increased formation of antiviral proteins

Interferon (TOPNOTCH)

For chronic HBV, HCV infection, Kaposi sarcoma, genital warts, prevents dissemination of HZV in cancer patients and decreased CMV shedding after renal transplantation

Interferon (TOPNOTCH)

Inhibits HBV DNA polymerase causing chain termination after incorporation into the viral DNA

Adefovir, Dipivoxil, Telbivudine, Tenofovir (TOPNOTCH)

______ is a prodrug of Adefovir

Dipiroxil (TOPNOTCH)

_____is an anti-RT drug that is also effective in chronic HBV, it is active against lamivudine and entecavir-resistant strains

Tenofovir (TOPNOTCH)

guanosine nucleoside, inhibits DNA polymerase

Entecavir (TOPNOTCH)

Coinfection between HBV and HIV may increase the risk of pancreatitis with_____use

lamivudine (TOPNOTCH)

Inhibits guanosine triphosphate formation, prevents capping of viral mRNA, blocks RNA-dependent RNA polymerase, inhibit replication of many DNA and RNA viruses like Influenza A and B, parainfluenza, paramyxo viruses, HCV and HIV

Ribavirine (TOPNOTCH)

For HCV infection (with IFN ) and RSV infection, decreasesmortality in viral hemorrhagic fevers

Ribavirine (TOPNOTCH)

Prevents polymerization of heme into hemozoin, blood schizonticide

Chloroquine, hydroxychloroquine (TOPNOTCH)

Complexes with DNA to prevent strand separation, blocks DNA replication and transcription, blood schizonticide

Quinine, quinidine gluconate (TOPNOTCH)

DOC for malaria in pregnant patients

Quinine, quinidine gluconate (TOPNOTCH)

1st line drug (weekly administration) for prophylaxis in all areas with Chloroquine resistance)

Mefloquine (TOPNOTCH)

Forms electron-transferring redox compounds that act as cellular oxidants, tissue schizonticides, gametocides

Primaquine (TOPNOTCH)

Eradicates hypnozoites in the liver, preventing malarial relapse

Primaquine (TOPNOTCH)

______ disrupts mitochondrial electron transport, blood and tissue schizonticide, ______ inhibits folate synthesis, sporonticide

Atovaquone-proguanil (TOPNOTCH)

also effective against Mefloquine-resistant Falciparum infection

Atovaquone-proguanil (TOPNOTCH)

_____ is the DOC for uncomplicated falciparum malaria in the Philippines

Co-artem (TOPNOTCH)

DOC for asymptomatic cyst carrier of E. histolytica

Diloxanide Furoate (TOPNOTCH)

Inhibits protein synthesis, blocks ribosomal movement along messenger RNA, tissue amebicide ; back up drug for severe intestinal and extraintestinal amebiasis

Emetine, dehydroemetine (TOPNOTCH)

Inhibits protein synthesis, binds to 16S ribosomal subunit, luminal amebicide ; For intestinal amebiasis, cryptosporidiosis

Paromomycin (TOPNOTCH)

For metronidazole-resistant amebiasis, giardiasis, cryptosporidiosis (DOC)

Nitazoxanide (TOPNOTCH)

For prophylaxis and treatment of pneumocystosis (DOC), prophylaxis (T. gondii, I. belli)

Co-trimoxazole (TOPNOTCH)

For prophylaxis and treatment of toxoplasmosis (DOC)

Pyrimethamine-sulfadiazine (TOPNOTCH)

alternative drug for Toxoplasmosis is _____

Clindamycin (TOPNOTCH)

For African sleeping sickness (hemolymphatic stage),onchocerciasis (backup)

Suramin (TOPNOTCH)

Suicide inhibitor of ornithine decarboxylase; For advanced west African sleeping sickness (DOC)

Eflornithine (TOPNOTCH)

Organic arsenical, inhibits enzyme sulfhydryl groups in trypanosomes; DOC for African sleeping sickness

Melarsoprol (TOPNOTCH)

Inhibits trypanothione reductase; DOC for Chagas disease (Trypanosoma cruzi)

Nifurtimox (TOPNOTCH)

DOC for Leishmaniasis

Sodium Stibogluconate (TOPNOTCH)

Selectively inhibits microtubule synthesis and glucose uptake in nematodes, ovicidal ; For ascariasis, pinworm, whipworm

Mebendazole (TOPNOTCH)

Inhibits microtubule assembly, larvicidal and ovicidal ; For ascariasis, hookworm, whipworm, hydatid disease (DOC), threadworms, filariasis, larva migrans, cysticercosis

Albendazole (TOPNOTCH)

primary drug for ascariasis, ancylostomiasis, trichuriasis

Albendazole (TOPNOTCH)

DOC for filariasis and eye worm disease

Diethylcarbamazine (TOPNOTCH)

May cause mazzotti reaction when used for onchocerciasis

Diethylcarbamazine (TOPNOTCH)

Intensifies GABA-mediated neurotransmission in nematodes, immobilizes parasites ; DOC for strongyloidiasis

Ivermectin (TOPNOTCH)

Stimulates nicotinic receptors at NMJ of nematodes, causes depolarization-induced paralysis

Pyrantel pamoate (TOPNOTCH)

DOC for hookworm and roundworm infections

Pyrantel pamoate (TOPNOTCH)

DOC for trichinosis

Thiabendazole (TOPNOTCH)

DOC for trematodes (schistosoma, paragonimus, clonorchis, opistorchis) and cestodes (taenia, diphyllobothrium)

Praziquantel (TOPNOTCH)

Used with steroid when treating neurocysticercosis, contraindicated in ocular cysticercosis (may cause irreparable eye damage)

Praziquantel (TOPNOTCH)

Increases membrane permeability to calcium, cause muscle paralysis, vacualization and death

Praziquantel (TOPNOTCH)

Uncouples oxidative phosphorylation or by activating ATPases ; alternative drug for cestode infection (Taenia, diphyllobotrium)

Niclosamide (TOPNOTCH)

Forms DNA cross-links, resulting in inhibition of DNA synthesis and function, Cell-cycle nonspecific

Alkylating agents (TOPNOTCH)

Alkylating agents

Cyclophosphamide, chlorambucil, Cisplatin, Carboplatin, oxaliplatin, Procarbazine, Dacarbazine, Busulfan, Carmustine, lomustine (TOPNOTCH)

SE: bone marrow suppression, hemorrhagic cystitis, hepatotoxicity, alopecia, SIADH, pulmonary toxicity

Cyclophosphamide (TOPNOTCH)

Rescue therapy for cyclophosphamide

MESNA (TOPNOTCH)

Rescue therapy for Cisplatin

Amifostine (TOPNOTCH)

can penetrate the CSF, For Hodgkin's lymphoma, non-hodgkin's lymphoma, brain tumors

Procarbazine (TOPNOTCH)

SE: pulmonary fibrosis, adrenal insufficiency, skin pigmentation

Busulfan (TOPNOTCH)

Highly lipophilic allowing ease of passage through BBB into the CNS ; For brain tumors, melanoma, skin cancer

Carmustine, lomustine (TOPNOTCH)

Inhibits dihydrofolate reductase, decreases synthesis of thymidylate, amino acids, purine nucleotides; cell cycle specific

Methotrexate (TOPNOTCH)

Rescue therapy for methotrexate

Leucovorin (Folinic acid) (TOPNOTCH)

Inhibits de novo purine nucleotide synthesis, activated by HGPRT, cell cycle specific ; For acute leukemia (AML, ALL), CML

6-Mercaptopurine, 6-thioguanine, fludarabine, cladribine (TOPNOTCH)

Inhibits thymidylate synthase, causes thymineless death of cells, cell cycle specific

5-Fluorouracil (TOPNOTCH)

a deoxycytidine analog

Gemcitabine (TOPNOTCH)

Most specific for the S-phase of the cell cycle

Cytarabine (TOPNOTCH)

Prevents microtubule assembly, causes cell arrest at metaphase, cell cycle specific

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

Inhibits DNA topoisomerase II, inhibits mitochondrial electron transport, cell cycle specific

Etoposide (TOPNOTCH)

Inhibits DNA topoisomerase I, cell cycle specific; For advanced ovarian cancer (2nd line), small cell lung cancer

Topotecan, irinotecan (TOPNOTCH)

Interferes with mitotic spindle, prevents microtubule disassembly into tubulin monomers, cell cycle specific

Paclitaxel, docetaxel (TOPNOTCH)

used in solid tumors like breast, ovarian, lung, gastroesophageal, prostate, bladder and head & neck cancers

Paclitaxel, docetaxel (TOPNOTCH)

Acts primarily in M phase of cancer cell cycle

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

Intercalates between base pairs, inhibits topoisomerase II, generates free radicals cell cycle non-specific

Anthracycline: Doxorubicin, daunorubicin, idarubicin, epirubicin, mitoxantrone (TOPNOTCH)

Rescue therapy for Doxorubicin

dexrazoxane (TOPNOTCH)

Most specific for the G2 phase of cell cycle

Bleomycin (TOPNOTCH)

SE: pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous reactions

Bleomycin (TOPNOTCH)

Binds to double stranded DNA, inhibits DNA-dependent RNA synthesis, cell cycle non-specific

Actinomycin D (TOPNOTCH)

Tyrosine kinase inhibitor of the protein product of bcr-abl oncogene in CML ; For CML, GIST

TK inhibitor: Imatinib, dasatinib, nilotinib (TOPNOTCH)

recognizes a surface protein in breast CA cells that overexpress Her-2-Neu receptors for epidermal growth factor

Trastuzumab (TOPNOTCH)

Inhibits binding of VEGF to VEGFR leading to inhibiton of VEGF signalling, inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

Bevacizumab (TOPNOTCH)

Binds to a surface protein in NHL cells, induces complement-mediated lysis, direct cytotoxicity and induction of apoptosis

Rituximab (TOPNOTCH)

Endogenous glycoproteins with antineoplastric, immunosuppressive and antiviral actions

Interferon alpha (TOPNOTCH)

Depletes serum asparagines ; For ALL, T-cell auxotrophic CA (leukemia and lymphomas) that require asparagine for growth

Asparaginase (TOPNOTCH)

Only vitamin that can cure cancer

All-Trans retinoic acid (TOPNOTCH)

For acute promyelocytic leukemia

All-Trans retinoic acid (TOPNOTCH)

Suppresses inflammation and immune response, may trigger apoptosis and work on nondividing cancer cells

Prednisone (TOPNOTCH)

Estrogen antagonist actions in breasts tissue and CNS, estrogen agonist effects in uterus, liver and bone

Tamoxifen (TOPNOTCH)

Androgen antagonist ; For prostate cancer

Flutamide (TOPNOTCH)

Increased LH, FSH secretion with intermittent administration, reduced LH and FSH secretion with prolonged continuous administration ; For prostate cancer

Leuprolide (TOPNOTCH)

Reduces estrogen synthesis by inhibiting aromatase; For breast cancer

Anastrazole (TOPNOTCH)

Effective againsts breast cancer that have become resistant to tamoxifen

Anastrazole (TOPNOTCH)

Neutralize stomach acid by reacting with protons in the lumen

Antacids (TOPNOTCH)

Impairs absorption of tetracyclines, flouroquinolones,itraconazole and iron

Antacids (TOPNOTCH)

Antacids

Magnesium-Aluminum Hydroxide, Calcium carbonate, Sodium bicarbonate (TOPNOTCH)

Competitive pharmacologic block of H2 receptors ; for peptic ulcer disease, Zollinger-Ellison syndrome, Gastroesophagal reflux, dyspepsia

H2 Receptor Blockers (TOPNOTCH)

H2 Receptor Blockers

Cimetidine, Ranitidine, Famotidine, Nizatidine (TOPNOTCH)

Highly effective in suppressing nocturnal acid secretion but only modest effect on meal- stimulated secretion

H2 Receptor Blockers (TOPNOTCH)

Irreversible blockade of H/K ATPase in active gastric panetal cells. Long lasting reduction of meal stimulated and nocturnal acid secretion

Proton Pump Inhibitors (TOPNOTCH)

Proton Pump Inhibitors

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

usually enetric coated, needs 3-4 days treatment to achieve full effectiveness

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

SE: Diarrhea, headache, abdominal pain, Malaabsorption (Vit B12, Ca, Fe, Zn), Infections (respiratory, enteric), Hypergastrinemia, Atrophic gastritis

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

Binds to injured tissue and forms a protective covering with ulcer beds. Accelerates healing of peptic ulcers and reduces recurrence rate

Sucralfate (TOPNOTCH)

Forms a protective coating on ulcerated tissue. Stimulates mucosal protective mechanisms, direct antimicrobial effects and sequestration of enterotoxins

Bismuth Salicylate (TOPNOTCH)

SE: Abdominal pain, Diarrhea, Uterine cramping, Miscarriage

Misoprostol (TOPNOTCH)

Activates EP receptors. Causes incresed HCO3 and mucus secretion in stomach. Uterine contraction

Misoprostol (TOPNOTCH)

SE: Black stools, darkening of tongue, Encephalopathy (Atraxia, headaches, confusion, seizures)

Bismuth Salicylate (TOPNOTCH)

Increases gastric emptying and intestinal motility

Metoclopramide, Domperidone, Erythromycin (TOPNOTCH)

______ and ______ block D receptors ; _______ stimulates motilin receptors

Metoclopramide and domperidone, Erythromycin (TOPNOTCH)

T or F: Domperidone does not cross the BBB (less toxic)

TRUE (TOPNOTCH)

Indigestible, hydrophilic colloids that absorb water, forming a bulky emollient gel that distends the colon and promotes peristasis

Bulk-forming Laxatives: Psyllium, Methylcellulose, Polycarbophil (TOPNOTCH)

Soften stool material, Permitting water and lipids to penetrate

Stool-softener: Docusate, Glycerine, Suppository, Mineral oil (TOPNOTCH)

Soluble but nonabsorbable compound that result in increased stool liquidity due to an obligate increase in fecal fluid

Osmotic Laxatives: Lactulose, Magnesium oxide, Sorbitol, Magnesium citrate, Sodium phosphate, Polyethylene Glycol (TOPNOTCH)

Directly stimulate enteric nervous system and colonic electrolyte and fluid secretion

Stimulant Laxatives: Bisacodyl, Aloe, Senna, Cascara, Castor oil (TOPNOTCH)

Activates opioid receptors in enteric nervous system. Slows motility with negligible CNS effects

Diphenoxylate, Loperamide, Kaolin+Pectin, Colloidal Bismuth (TOPNOTCH)

Blocks chemoreceptor trigger zone and enteric nervous system 5-HT3 receptors ; For Vomiting (Post chemothereaphy, postoperative)

Ondansetron, Granisetron, Dolasetron, Palonosetron (TOPNOTCH)

Probably inhibits production of eicosanoid inflammatory mediators ; for Inflammatory bowel disease (mild to moderate)

Mesalamine, Balsalazide, Olsalazine, Sulfasalazine (TOPNOTCH)