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)
