Pharmacology Flashcards
rapidly hydrolyzed by AChE
Acetylcholine (TOPNOTCH)
resistant to AChE
Betanechol (TOPNOTCH)
for Bladder and bowel atony
Betanechol (TOPNOTCH)
Nonselective muscarinic and nicotinic agonist , used topically for glaucoma treatment
Carbachol (TOPNOTCH)
Partial muscarinic agonist; used for treatment of Glaucoma, Sjogren’s syndrome and Sicca syndrome
Pilocarpine (TOPNOTCH)
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)
activates autonomic post ganglionic neurons (both sympathetic and parasympathetic) and skeletal muscle neuromuscular end plants
Nicotine(TOPNOTCH)
used exclusively for smoking cessation
Varenicline (TOPNOTCH)
for Myasthenia gravis diagnosis (Tensilon test)
Edrophonium (TOPNOTCH)
for Myasthenia gravis treatment; reversal of nondepolarizing muscular blockade
Neostigmine (TOPNOTCH)
Long Acting Cholinesterase Inhibitors used as Scabicide and Insecticide
Malathion, Parathion (TOPNOTCH)
Competitively blocks all muscarinic receptors, antagonizes histamine and serotonin ; for motion sickness, dec. acid secretion in the GIT
Scopolamine (TOPNOTCH)
DOC for organophosphate poisoning
Atropine (TOPNOTCH)
for bradycardia, hypersalivation and to decrease airway secretion during general anesthesia
Atropine (TOPNOTCH)
Mydriatic, cycloplegic in eye examinations
Homatropine, Cyclopentolate, Tropicamide (TOPNOTCH)
Competitive nonselective antagonist at muscarinic receptors ; for BA and COPD, not as effective as SABAs but less tachycardia and arrhythmia
Ipratropium, Tiotropium (TOPNOTCH)
Nonselective muscarinic antagonist which reduces detrussor smooth muscle tone spasms
Oxybutinin (TOPNOTCH)
for decreasing urgency in mild cystitis and dec. bladder spasm after urologic surgery
Oxybutinin (TOPNOTCH)
Usual antidote for early stage (48h) cholinesterase inhibitor poisoning, Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs
Pralidoxime (TOPNOTCH)
Competitively blocks all Nn nicotinic Ach receptors ; for Hypertensive emergencies (obsolete)
Hexamethonium, Mecamylamine, Trimethaptan (TOPNOTCH)
DOC for Anaphylaxis
Epinephrine (TOPNOTCH)
used for Cardiac arrest, anaphylaxis, asthma, COPD, Hemostasis
Epinephrine (TOPNOTCH)
for cardiogenic Shock and heart failure
Norepinephrine (TOPNOTCH)
causes vasodilation in splanchnic and renal blood vessels ; for cardiogenic Shock and heart failure
Dopamine (TOPNOTCH)
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)
