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January 21, 2014

#PharMasaya

Baby Katzung

(2nd Shifting Reviewer)

"Realize that if you have time to whine and complain about something, then you have the
time to do something about it." Anthony J. D'Angelo

WALKTHROUGH
MAJOR DRUG CLASS
Notes on the major drug class above (if any)
DRUG
Notes on the drug subclass on the left side
SUBCLASS
DRUG
o Specific information
DRUG
Specific information
LECTURER
LOYOLA
ALABASTRO
FILARCA
DIMAANO
TORRES

FAVORITE QUESTIONS
Basic physiology, mechanism of action
Emphasized parts in pharmacokinetics, clinical uses, toxicity
Clinical uses, toxicity
Clinical uses, toxicity, contraindications
Drug of choice, toxicities (Di halata. Hahahaha.)
SECOND SHIFTING
GASTROINTESTINAL PHARMACOLOGY
ACID-PEPTIC DISEASES

ANTACIDS
Given 1 hour after meals
Short-acting (1-2 hours)
Cautions: renal insufficiency
Interactions: affect drug absorption by binding to other drugs or altering
intragastric pH
SODIUM
HCL CO2 + NaCl
BICARBONATE NaHCO3: renal insufficiency metabolic alkalosis
CO2: gastric distention, belching
NaCl: heart failure, hypertension, renal insufficiency
fluid retention
MAGNESIUM
MgCl2: osmotic diarrhea
HYDROXIDE +
AlCl3: constipation
ALUMINUM
No gas formation no belching
HYDROXIDE
Reacts with HCl forms protective viscous foam
ALGINATE
Clinical uses: heartburn, GERD

H2 RECEPTOR ANTAGONISTS ("tidine")

Highly selective competitive antagonist at parietal cell H2 receptor
Extremely safe (few adverse effects)
Pharmacokinetics: long-acting (6-10 hours), given BID
Clinical uses: prophylaxis of heartburn, PUD, stress-related gastritis
No CYP450 interactions: famotidine, nizatidine
CIMETIDINE
Toxicity: mental status changes, gynecomastia, impotence,
galactorrhea, bradycardia, hypotension
Interactions: CYP1A2, CYP2C9, CYP2D6, CYP3A4
RANITIDINE
Less affinity to CYP450 than cimetidine
FAMOTIDINE blood ethanol
NIZATIDINE
Little first-pass metabolism
~100% bioavailability
PROTON PUMP INHIBITORS ("prazole")
Substituted benzoimidazoles, inactive prodrugs
Active metabolite: sulfonamide cation irreversibly inactivates proton
pump (H+/K+-ATPase)
Given BID on empty stomach to absorption
Formulated as acid-resistant enteric-coated tablets or capsules
Concentrated in parietal cell canaliculi (site of action) by HendersonHasselbach trapping
Short t1/2 (1.5 hours), long-acting (24 hours)
DOC for acid-peptic diseases
o GERD and Barrett esophagus

o Triple therapy in H. pylori-associated peptic ulcers (10-14 day

regimen of PPI + clarithromycin + amoxicillin/metronidazole)
o NSAID-associated ulcers
o Gastrinomas and hypersecretion
Toxicity: B12 and electrolyte absorption, risk of nosocomial infections,
hypergastrinemia
OMEPRAZOLE
Formulated as non-enteric-coated powder

SUCRALFATE

MISOPROSTOL

BISMUTH
SUBSALICYLATE

MUCOSAL PROTECTANTS
Reacts with water or acid forms viscous paste
Negatively-charged sucrose sulfate binds to positivelycharged proteins on ulcers
Alternative to acid-inhibitory therapies (less risk of
nosocomial infections)
Cautions: renal insufficiency
PGE1 analog stimulates mucus and HCO3 secretion,
acid
DOC for NSAID-induced ulcers
Toxicity: diarrhea, abdominal pain, abortifacient
Coats ulcers and erosions
Binds enterotoxins
Clinical uses: traveler's diarrhea, H. pylori (second-line)
Toxicity: harmless black stool, encephalopathy,
salicylate toxicity

GASTROPROKINETIC AGENTS
Selectively stimulate gut motor function
LES pressure (useful in GERD)
GI emptying (useful in gastroparesis, post-vagotomy/antrectomy)
BETHANECHOL
o Stimulates M3 receptors on GIT smooth muscle and
CHOLINERGIC
at myenteric plexus synapses
AGENTS
NEOSTIGMINE
o Clinical uses: Ogilvie syndrome (acute colonic
pseudo-obstruction)
Clinical uses: GERD, gastroparesis, antiemetic,
postpartum lactation
METOCLOPRAMIDE
D2 RECEPTOR
o Toxicity: extrapyramidal symptoms
ANTAGONISTS
DOMPERIDONE
o Promotes postpartum lactation
o Toxicity: hyperprolactinemia
ERYTHROMYCIN
o Stimulates motilin receptors and facilitates MMC
MACROLIDES
o Clinical uses: pre-endoscopy evacuation of blood in
patients with UGIB
CONSTIPATION
LAXATIVES
Clinical uses: colonic evacuation in constipated patients
BULK Indigestible hydrophilic colloids
FORMING
Form emollient gel colonic distention, hyperperistalsis
LAXATIVES
Bacterial digestion of fiber bloating, flatulence
PSYLLIUM, METHYLCELLULOSE
STOOL
Given PO or rectally
SURFACTANTS Minimize straining
DOCUSATE
o Commonly prescribed stool surfactant
MINERAL OIL
o Lubricates feces and retards water absorption
o Clinical uses: fecal impaction in children and

Page 1 of 13

Baby Katzung (Finals Reviewer)

OSMOTIC
LAXATIVES

STIMULANT
LAXATIVES

CHLORIDE
CHANNEL
ACTIVATORS

OPIOID
RECEPTOR
ANTAGONISTS

5-HT4
RECEPTOR
AGONISTS

PROKINETIC
BENZAMIDES

GUANYLATE
CYCLASE C
AGONISTS

debilitated adults
o Aspiration lipid pneumonitis
o Prolonged use: vitamin malabsorption
NON-ABSORBABLE SUGARS OR SALTS
o Clinical uses: treatment of acute constipation,
prevention of chronic constipation
BALANCED POLYETHYLENE GLYCOL
MAGNESIUM HYDROXIDE (MILK OF MAGNESIA)
o Most commonly used osmotic laxative
o Prolonged use: hypermagnesemia in renal
insufficiency
LACTULOSE
o DOC for hepatic encephalopathy
o Metabolized by bacteria flatus, cramps
MAGNESIUM CITRATE AND SODIUM PHOSPHATE
o Purgatives
o Toxicity: hypovolemia, electrolyte fluctuations
BALANCED POLYETHYLENE GLYCOL
o Lavage solution of PEG and electroytes
o Clinical uses: pre-endoscopy colonic cleansing
Direct ENS stimulation + colonic electrolyte and fluid
secretion colonic movement
ANTHRAQUINONE DERIVATIVES (ALOE, SENNA,
CASCARA)
o Chronic use: melanosis coli
DIPHENYLMETHANE DERIVATIVES (BISACODYL)
o Clinical uses: acute and chronic constipation, preendoscopy cleansing
Stimulate type 2 Cl- channels in small intestine Clsecretion GI motility, transit time
LUBIPROSTONE
o Prostanoic acid derivative
Inhibit GIT -opioid receptors
METHYLNALTREXONE
o Opioid-induced constipation
ALVIMOPAN
o Post-bowel resection ileus
Stimulate 5-HT4 receptors in submucosal plexus
TEGASEROD
o High affinity partial agonist
o Withdrawn due to risk of CV events
CISAPRIDE
o Partial agonist
o Inhibits hERG QT prolongation
PRUCALOPRIDE
o High affinity agonist
o Clinical uses: chronic constipation in women
ITOPRIDE
o Inhibits D2 receptors and acetylcholinesterase
o gastric emptying time
LINACLOTIDE
o Binds to guanylate cyclase C receptor on enterocyte
luminal surface CFTR activation fluid
secretion
DIARRHEA

ANTIDIARRHEALS
Clinical uses: mild to moderate acute diarrhea
Cautions: bloody diarrhea, hyperthermia, systemic toxicity
OPIOID
Inhibit presynaptic cholinergic neurons in enteric
AGONISTS
plexuses colonic transit time, mass movement
No analgesic property
LOPERAMIDE
o No CNS entry
DIPHENOXYLATE
o CNS effects

#PharMasaya :P

BILE-SALT
SEQUESTRANTS

SOMATOSTATIN
ANALOGS

OTHERS

o Prolonged use: dependence (combined with

atropine to discourage dependence)
fecal excretion of bile acids
Toxicity: bloating, flatulence, constipation, fat
malabsorption
COLESEVELAM
o No drug interactions
OTHERS (COLESTIPOL, CHOLESTYRAMINE)
OCTREOTIDE
o Inhibits GIT hormone and neurotransmitter
secretion antimotility effect
o Clinical uses: diarrhea 2 to hypersecretion, postvagotomy, dumping syndrome, VIPoma
o Toxicity: steatorrhea (2 to impaired pancreatic
secretion), alterations in GI motility, acute
cholecystitis, hyperglycemia
BISMUTH
KAOLIN (ATTAPULGITE) AND PECTIN
o Absorb bacteria, toxins, fluids stool liquidity
o Clinical uses: acute diarrhea
IRRITABLE BOWEL SYNDROME

ANTISPASMODICS
DICYCLOMINE, HYOSCYAMINE
o Inhibit muscarinic cholinergic receptors
5-HT3 RECEPTOR ANTAGONISTS ("setron")
5-HT3 receptor blockade in enteric terminals motility
ALOSETRON IBS with predominant diarrhea in women
Toxicity: GI toxicity, constipation, ischemic colitis

TEGASEROD

5-HT4 RECEPTOR AGONISTS

IBS with predominant constipation in women

LUBIPROSTONE

CHLORIDE CHANNEL ACTIVATORS

IBS with predominant constipation in women
NAUSEA AND VOMITING

5-HT3 RECEPTOR ANTAGONISTS ("setron")

ONDANSETRON, GRANISETRON, DOLASETRON, PALONOSETRON
o Potent antiemetic properties
Peripheral 5-HT3 blockade in extrinsic intestinal neurons
Central 5-HT3 blockade in chemoreceptor trigger zone
o Clinical uses: post-operative and post-radiation N/V
o DOC for acute chemotherapy-induced N/V (CINV)
o Not used in delayed CINV
o Toxicity: headache, dizziness, constipation
PALONOSETRON Newer IV agent
Higher affinity to 5-HT3 receptor
Long-acting (t1/2: 40 hours)
DOLASETRON
QT prolongation
CORTICOSTEROIDS WITH ANTIEMETIC ACTIVITY
DEXAMETHASONE, METHYLPREDNISONE
o Enhance efficacy of 5-HT3 receptor antagonists
o Clinical uses: prevention of acute and delayed CINV

APREPITANT

NEUROKININ (NK1) RECEPTOR ANTAGONISTS

Central blockade in area postrema
Metabolized by CYP3A4
Combined with 5-HT3 receptor antagonists and steroids
Clinical uses: acute and delayed CINV

Page 2 of 13

Baby Katzung (Finals Reviewer)

DOPAMINERGIC ANTAGONISTS
Toxicity: mental status changes, extrapyramidal symptoms
PHENOTHIAZINES
PROMETHAZINE, PROCHLORPERAZINE,
THIETHYLPERAZINE
o Potent antiemetic and sedative activity
BUTYROPHENONES
DROPERIDOL
o Clinical uses: post-operative N/V
o Toxicity: extrapyramidal symptoms,
hypotension, QT prolongation
PROKINETICS
TRIMETHOBENZAMIDE, METOCLOPRAMIDE
ANTICHOLINERGIC H1 ANTIHISTAMINES
Weak antiemetic activity
Clinical uses: motion sickness
SCOPOLAMINE
DOC for motion sickness
DIPHENHYDRAMINE
Potent sedative
MECLIZINE
Minimal anticholinergic and sedating effects
DOC for vertigo

LORAZEPAM,
DIAZPEAM

DRONABINOL

BENZODIAZEPINES
Given pre-chemotherapy to reduce anticipatory vomiting

CANNABINOIDS ("nabi")
THC analog
Clinical uses: antiemetic, appetite stimulant
Interactions: phenothiazines (synergistic effect,
attenuates adverse effects of both)
Toxicity: sedation, euphoria, dysphoria, hallucination,
ANS effects
INFLAMMATORY BOWEL DISEASE

AMINOSALICYLATES (5-ASA)
5-aminosalicylic acid
Inhibits COX, nuclear factor-B, lymphocyte function
Pharmacokinetics: rapidly absorbed from proximal small intestine, Nacetylated to inactive metabolite in GIT epithelium and liver
DOC for mild to moderate IBD
AZO
5-ASA bound by azo bond (N=N) to inert compound or to
COMPOUNDS
another 5-ASA molecule
("salazine")
SULFASALAZINE
o 5-ASA + sulfapyridine
BALSALAZIDE
o 5-ASA + 4-aminobenzoyl--alanine
OLSALAZINE
o 2 molecules of 5-ASA
MESALAMINE
PENTASA
COMPOUNDS
o Small intestine
ASACOL, APRISO
o Distal ileum, proximal colon
LIALDA
o Colon
ROWASA (enema), CANASA (suppository)
o Rectum, sigmoid colon
PREDNISONE
HYDROCORTISONE
BUDESONIDE

GLUCOCORTICOIDS
Most commonly used
Topical treatment of active IBD in rectum and
sigmoid colon
Potent synthetic analog of prednisolone
High affinity glucocorticoid receptor agonist

ANTIMETABOLITES
Clinical uses: induction and maintenance of remission in ulcerative colitis
and Crohn's disease
Toxicity: myelosuppression (leukopenia, anemia)
AZATHIOPRINE
Nonenzymatically converted to 6-MP inhibits purine
metabolism and DNA synthesis
T-lymphocyte apoptosis
Toxicity: N/V, hepatotoxicity
Pre-therapy monitoring: TPMT activity
Interactions: allopurinol (severe leukopenia)
METHOTREXATE Inhibits dihydrofolate reductase
ANTI-TNF MONOCLONAL ANTIBODIES
High affinity to TNF- prevent binding of TNF- to receptor
Clinical uses: treatment of acute and chronic moderate to severe Crohn's
disease and ulcerative colitis
Toxicity: infection, reactivation of latent TB, antibody formation
INFLIXIMAB
Chimeric mouse-human
Acute adverse infusion reactions
ADALIMUMAB
Fully humanized
CERTOLIZUMAB Pegylated Fab fragment

NATALIZUMAB

EXOCRINE PANCREATIC INSUFFICIENCY

PANCREATIC ENZYME SUPPLEMENTS
Toxicity: mucositis, hyperuricosuria, renal stones
PANCRELIPASE Greater lipolytic (X12) and proteolytic (X4) activity
compared to PANCREATIN
Creon: most common
GALLSTONES
URSODIOL (URSODEOXYCHOLIC ACID)
hepatic cholesterol secretion cholesterol content of bile
Clinical uses: dissolution of small gallstones, symptomatic gallbladder
disease, prevention of gallstones
liver function deviations and improves liver histology in biliary cirrhosis
ESOPHAGEAL VARICES
OCTREOTIDE
ARGININE
VASOPRESSIN

NONSELECTIVE
BETA BLOCKERS

HEMOSTATIC AGENTS
portal blood flow variceal pressure
Initial hemostasis
Splanchnic arterial vasoconstriction portal venous
pressure
Toxicity: CVS effects (hypertension, ischemia,
hyponatremia, pulmonary edema), GIT effects (nausea,
abdominal cramps, diarrhea)
TERLIPRESSIN
o Fewer adverse effects
PROPRANOLOL, NADOLOL
o portal inflow and portal venous pressure
o 2 blockade: splanchnic vasoconstriction
ALCOHOL PHARMACOLOGY

ETHANOL

#PharMasaya :P

ANTI-INTEGRIN
Humanized IgG4 monoclonal antibody
Blocks integrin prevents IgG binding to vascular
adhesion molecules
Clinical uses: moderate to severe Crohn's disease (if
other therapies fail)

ALCOHOLS
Water-soluble, rapidly absorbed in GIT in fasting state,
peaks in blood in 30 minutes, 90% oxidized in liver

Page 3 of 13

Baby Katzung (Finals Reviewer)

METHANOL

ETHYLENE
GLYCOL

DISULFIRAM

NALTREXONE

ACAMPROSATE

FOMEPIZOLE
OTHERS

Alcohol dehydrogenase
o Primary metabolic pathway of alcohol
o Converts alcohol to acetaldehyde
Microsomal ethanol oxidizing system
o Utilizes NADPH as cofactor
o Low affinity for alcohol
o Significantly active at BAC of >100 mg/dL
Aldehyde dehydrogenase
o Oxidizes acetaldehyde to acetate (further degraded
to CO2 + water)
Acute: sedation, anxiolysis, intoxication, memory loss,
myocardial contractility, vasodilation, hypothermia
Chronic: liver disease (fatty liver, alcoholic hepatitis,
cirrhosis), chronic pancreatitis, CNS effects (dependence,
Wernicke-Korsakoff), CVS effects (heart failure,
arrhythmia, hypertension, coronary diseases), endocrine
effects (steroid imbalance), fetal alcohol syndrome
Interactions: acetaminophen (hepatotoxicity), CNS
depressants (additive depression)
Metabolized by alcohol dehydrogenase
Metabolites: formaldehyde, formic acid, CO2
Toxicity: "snowstorm" vision, formalin breath, sudden
cessation of respiration
Management: respiratory support, hemodialysis,
alkalinization, ethanol and fomepizole
Metabolized to toxic aldehydes and oxalates
Same management in methanol poisoning
ANTI-ALCOHOLISM AGENTS
Alcohol dehydrogenase inhibitor
Provokes severe discomfort (flushing, N/V, sweating,
hypotension) after consuming alcohol
Interactions: alcohol-containing medications
Long-acting opioid receptor antagonist at -opioid
receptors
Interactions: disulfiram (hepatotoxicity), opioids
(withdrawal syndrome)
NMDA antagonist
GABAA receptor activator
Contraindications: renal impairment
Toxicity: N/V, vomiting, rashes
Alcohol dehydrogenase inhibitor
DOC for methanol or ethylene glycol poisoning
ONDANSETRON, TOPIRAMATE, BACLOFEN
o craving in chronic alcoholism
RIMONABANT
o CB1 receptor antagonist
o Suppresses alcohol-related behaviors
CENTRAL NEUROTRANSMITTERS

EXCITATORY

AMINO ACIDS
GLUTAMATE
o Taken up via vesicular glutamate transporter (VgluT)
o Released by Ca2+-mediated exocytosis
o Converted by glutamine synthetase to glutamine
(then converted to glutamine by glutaminase)
o Receptors
Ionotropic
AMPA: permeable to Na+ and K+
Kainic acid: expressed in hippocampus,
cerebellum, spinal cord
NMDA: present in all CNS neurons,
involved in long-term potentiation
Metabotropic (G protein-coupled)
Group I: postsynaptic
Group II: presynaptic

#PharMasaya :P

INHIBITORY

GAMMA-AMINOBUTYRIC ACID (GABA)

o Present in CNS in GABA-releasing interneurons
o Types
GABAA
Ionotropic
Fast component of inhibitory potentials
Activators: MUSCIMOL
Inhibitors: PICROTOXIN, BICUCULLINE
GABAB
Metabotropic (G protein-coupled)
Slow component of inhibitory potentials
Either inhibit Ca2+ channels or activate K+
channels
Activators: BACLOFEN
Inhibitors: 2-OH SACLOFEN
GLYCINE
o Interneurons in spinal cord and brainstem
o Inhibitors: STRYCHININE (potent spinal cord
proconvulsant)
SEDATIVE-HYPNOTICS

BENZODIAZEPINES ("zep", "zepam", "zolam")

7-membered heterocyclic ring with carboxamide group
Electronegative substituent at 7 position confers sedative-hypnotic activity
Bind to benzodiazepine site of GABAA receptor
frequency of channel-opening events
Cross placenta and breastmilk
Biotransformation: microsomal oxidation (phase I) catalyzed by CYP3A4
conjugation (phase II) to glucuronides
Toxicity: tolerance and dependence, anterograde amnesia,
cardiorespiratory depression
ANXIOLYTICS
All are long-acting except alprazolam and oxazepam
(short-acting)
Desmethyldiazepam
o Active metabolite of chlordiazepoxide,
clorazepate, and diazepam
ALPRAZOLAM
CHLORDIAZEPOXIDE, CLORAZEPATE
o Used in alcohol withdrawal
CLONAZEPAM
o No active metabolite
o Used in epilepsy
DIAZEPAM
o Used in epilepsy, alcohol withdrawal, and
muscle relaxation
o Alternative DOC for status epilepticus
OXAZEPAM
o Short-acting and no active metabolite
o Used in alcohol withdrawal
HYPNOTICS
ESTAZOLAM, FLURAZEPAM, QUAZEPAM,
TEMAZEPAM, TRIAZOLAM
o Used in sleep disorders
MIDAZOLAM
o Conscious sedation
ANXIOLYTIC LORAZEPAM
HYPNOTIC
o Intermediate-acting
o Used in delirium tremens
o DOC for status epilepticus
TRIAZOLES
Triazole ring at 1,2 position
Transformed to alpha-hydroxy metabolites
Short-acting
ALPRAZOLAM
o Used in panic attacks
TRIAZOLAM
o Used in sleep disorders

Page 4 of 13

Baby Katzung (Finals Reviewer)

Rapidly-absorbed: CLONed Dad, Father, Tatay (clonazepam, diazepam,

flurazepam, triazolam)
Active metabolites: FACT MD (flurazepam, alprazolam, chlordiazepoxide,
triazolam, midazolam, diazepam)
No active metabolites: CLOT (clonazepam, lorazepam, oxazepam,
temazepam)
Short-acting: TRI MO (triazoles, midazolam, oxazepam)
Intermediate-acting: LET (lorazepam, temazepam, estazolam)
Long-acting: everything else
BENZODIAZEPINE SUBTYPE
Generally rapid-acting
Metabolized by CYP3A4
Clinical uses: sleep disorders (insomnia)
ZALEPLON
Short-acting
Hydroxylation, oxidation (no active metabolite)
REM and latency of sleep
risk of tolerance
ZOLPIDEM
Ultra-short-acting
Aldehyde dehydrogenase (no active metabolite)
latency of sleep
Lowest risk of withdrawal symptoms
ESZOPICLONE Intermediate-acting
total sleep time
No rebound insomnia
BENZODIAZEPINE ANTAGONIST
1,4-benzodiazepine derivative
Competitive antagonist of benzodiazepines and
benzodiazepine subtype
High affinity to benzodiazepine site on GABAA receptor
Rapid-acting (t1/2: ~1 hour) sedation may recur
Clinical uses: BZ-induced CNS depression
Toxicity: severe abstinence syndrome
Interactions: tricyclics (seizures, arrhythmias)

FLUMAZENIL

BUSPIRONE

NON-BENZODIAZEPINES
Selective anxiolytic
Partial 5-HT1A agonist with affinity to D2 receptors
No depressant, anticonvulsant, relaxant properties
Active metabolite: 1-(2-pyrimidyl)-piperazine
Clinical uses: generalized anxiety state (not for panic
disorders)
Less risk of dependence and rebound anxiety

BARBITURATES ("barbital")
Bind to allosteric site on GABAA receptor
duration of channel-opening events
Clinical uses: sedation, hypnosis, anesthesia, anticonvulsant
Toxicity: cardiorespiratory depression
Contraindications: porphyria, hepatic and renal impairment
THIOPENTAL
Ultra-short-acting, very lipid-soluble (can enter CNS)
SECOBARBITAL
Short-acting (t1/2: 18 hours)
PENTOBARBITAL
Intermediate-acting (t1/2: 48 hours)
PHENOBARBITAL Long-acting (t1/2: 4-5 days)

RAMELTEON

MELATONIN RECEPTOR AGONISTS

MT1 and MT2 receptor agonist
Metabolized by CYP1A2
Clinical uses: maintenance of circadian rhythm, reduces
latency of sleep
No rebound effects or withdrawal symptoms
Cautions: hypertension and diabetes
Contraindications: hepatic impairment
Toxicity: mental status changes (dizziness, somnolence),
hyperprolactinemia

#PharMasaya :P

OTHER ANXIOLYTICS AND HYPNOTICS

Marked sedation
Long t1/2
ANTIDEPRESSANTS TRICYCLICS, MIRTAZAPINE, TRAZODONE
BETA BLOCKERS
Clinical uses: management of physiologic
components of anxiety (tachycardia, palpitations,
tremors, sweating)
No CNS depression and addiction
ANTIHISTAMINES

ANTIEPILEPTICS
PARTIAL AND GENERALIZED TONIC-CLONIC SEIZURES
ANTI-MAXIMAL ELECTROSHOCK CLASS
SODIUM CHANNEL BLOCKERS
Blocks voltage-gated Na+ channels (VGNC) high-frequency neuronal
firing (no effect on physiologic firing)
HYDANTOINS
PHENYTOIN
o Alters Na+, K+, and Ca2+ conductance
o glutamate release
o Exhibits non-linear kinetics
o High protein binding (99%)
o Toxicity: gingival hyperplasia, hirsutism
FOSPHENYTOIN
o Prodrug of phenytoin
TRICYCLICS
CARBAMAZEPINE
("zepine")
o DOC for complex partial seizures
o Active metabolite: carbamazepine-10,11 epoxide
o Toxicity: CNS effects (diplopia, ataxia),
hyponatremia
OXCARBAZEPINE
o Active metabolite: 10-hydroxy metabolite
MISCELLANEOUS
ZONISAMIDE
o Blocks VGNC and T-type Ca2+ channels
o Toxicity: renal stones
LACOSAMIDE
o Enhances slow inactivation of VGNC
o Binds to CRMP-2 neuronal growth
RUFINAMIDE
o Clinical uses: Lennox-Gastaut syndrome
(childhood-onset epilepsy)

RETIGABINE

POTASSIUM CHANNEL AGONISTS

K+ channel opening hyperexcitability
Toxicity: CNS effects (dizziness, somnolence, confusion,
blurred vision, dysarthria)

BENZODIAZEPINES

BARBITURATES

GABA ANALOGS
("gaba")

GABA AGONISTS
DIAZEPAM
LORAZEPAM
o Longer-acting than diazepam
o DOC for status epilepticus
PHENOBARBITAL
o inhibitory and excitatory transmission
o DOC for seizure in infants, also used in febrile
seizures
PRIMIDONE
o Active metabolites: phenobarbital,
phenylethylmalonamide (PEMA)
VIGABATRIN
o Irreversibly inhibits GABA aminotransferase
GABA degradation GABA levels
o DOC for infantile spasms (West syndrome)
o Toxicity: drowsiness, dizziness
o Prolonged use: visual field defects
o Contraindications: psychosis

Page 5 of 13

Baby Katzung (Finals Reviewer)

GABAPENTIN
o Enters CNS via L-amino acid transporter
o Modifies release of GABA
o Clinical uses: dystonia, migraine
PREGABALIN
o Clinical uses: fibromyalgia
TIAGABINE
o Inhibits GABA uptake in neurons and glia
o Prolongs inhibitory action of synapticallyreleased GABA
o Toxicity: cognitive slowing
PLEIOTROPICS
Multiple mechanisms of action
Clinical uses: partial seizures
LAMOTRIGINE
Suppresses sustained rapid firing
Voltage- and use-dependent inactivation of Na+
channels
Inhibits voltage-gated N and P/Q Ca2+ channels
Bipolar disorder
Toxicity: skin rash
LEVETIRACETAM
Binds to synaptic vesicular protein SV2A glutamate
FELBAMATE
Use-dependent block of NR1-2B NMDA receptor
Blocks strychnine-insensitive glycine site on NMDA complex
TOPIRAMATE
AMPA receptor antagonist
ABSENCE SEIZURES
ANTI-PENTYLENETETRAZOL CLASS
CALCIUM CURRENT INHIBITORS
T-type Ca2+ current in thalamic neurons
Clinical uses: absence seizures
SUCCINIMIDES
ETHOSUXIMIDE
o DOC for absence seizures
MISCELLANEOUS
VALPROIC ACID
o K+ channel agonist
o Blocks voltage-gated Na+ channel
o Blocks NMDA receptor-mediated excitation
o Facilitates glutamic acid decarboxylase
GABA synthesis
o High protein binding
o Displaces phenytoin from plasma proteins
o DOC for Lennox-Gastaut syndrome
o Second line for absence seizures
o Toxicity: hepatotoxicity, spina bifida
OXAZOLIDINEDIONES TRIMETHADIONE
o seizure threshold
o Active metabolite: dimethadione
o Toxicity: sedation
OTHER ANTIEPILEPTICS
CARBONIC ANHYDRASE
INHIBITORS
HORMONES

ACETAZOLAMIDE
o Produces mild acidosis in the brain
anticonvulsant effect
PROGESTERONE

CARBIDOPA
SINEMET
STALEVO

Prolonged use: fluctuations in response

o Wearing-off reaction: timing-related
o On-off phenomenon: characterized by "off" periods of
akinesia with "on"periods of dyskinesia, non-timingrelated
Interactions: MAOA inhibitors (hypertensive crisis)
Peripheral dopa decarboxylase inhibitor
L-dopa metabolism available L-dopa for CNS
LEVODOPA + CARBIDOPA
LEVODOPA + CARBIDOPA + ENTACAPONE

DOPAMINE RECEPTOR AGONISTS

Monotherapy in younger patients
No toxic metabolites
incidence of fluctuations
Toxicity: GIT effects (N/V, anorexia), dyskinesias, mental disturbances
ERGOT
BROMOCRIPTINE
DERIVATIVES
o D2 agonist
PERGOLIDE
o D1 and D2 agonist
o "on" periods in fluctuators
o Toxicity: cardiac valvulopathies
NON-ERGOT
PRAMIPEXOLE
DERIVATIVES
o D3 agonist
ROPINIROLE
o D2 agonist
o Metabolized by CYP1A2
APOMORPHINE
o Pharmacokinetics: SQ route, rapid absorption
o Clinical uses: temporary relief (rescue) from "off"
periods of akinesia
o Toxicity: persistent nausea
o Pre-therapy: trimethobenzamanide (anti-nausea)
SELECTIVE MONOAMINE OXIDASE B INHIBITORS ("giline")
Clinical uses: mild parkinsonism or children with parkinsonism
Interactions: L-dopa or tyramine (hypertensive crisis), SSRI or tricyclic
antidepressants (serotonin syndrome)
Contraindications: analgesics, OTC cold medications
SELEGILINE
Inhibits MAOA at high doses
on-off or wearing-off fluctuations
Metabolites: desmethylselegiline (neuroprotective),
amphetamines (causes adverse effects)
RASAGILINE Early symptomatic treatment of Parkinson
CATECHOL-O-METHYLTRANSFERASE INHIBITORS ("capone")
Clinical uses: severe parkinsonism or on-off phenomenon
ENTACAPONE Peripheral COMT inhibitor
No CNS entry
TOLCAPONE
Central and peripheral COMT inhibitor
Capable of CNS entry
Longer-acting, more potent
Toxicity: hepatotoxicity ( liver enzymes)

AMANTADINE

PARKINSON'S DISEASE
LEVODOPA
(L-DOPA)

DOPAMINE PRECURSORS
Enters CNS via L-amino acid transporter
Decarboxylated to dopamine
Extracerebral metabolism only 1-3% enters CNS
Metabolites: homovanillic acid (HVA),
dihydroxyphenylacetic acid (DOPAC)
Toxicity: GIT effects (N/V, anorexia), CVS effects
(arrhythmias, hypotension), dyskinesias

#PharMasaya :P

ANTICHOLINERGIC
AGENTS

OTHER ANTIPARKINSONIANS
Potentiates dopaminergic functions
Inhibits adenosine effects at adenosine A2A receptors
disinhibition of D2 receptor function
iatrogenic dyskinesias
Toxicity: mental status changes, livedo reticularis,
peripheral edema
BENZTROPIN, BIPERIDEN, ORPHENADRINE,
PROCYCLIDINE, TRIHEXYPHENIDYL
o Muscarinic receptor antagonists in basal ganglia
o tremors and rigidity
o Little effect on bradykinesia

Page 6 of 13

Baby Katzung (Finals Reviewer)

THERAPY FOR NON-MOTOR MANIFESTATIONS OF PARKINSON

RIVASTIGMINE, MEMANTINE, DONEPEZIL Cognitive decline (dementia)
ANTIDEPRESSANTS, ANXIOLYTICS
Affective disorders
MODAFINIL
Excessive daytime sleepiness
DEPRESSION AND ANXIETY DISORDERS
SELECTIVE SEROTONIN REUPTAKE INHIBITORS
Highly selective SERT blockade
Little effect on NET and adrenoceptors
All protein-bound and highly lipophilic
Potent CYP2D6 inhibitors: fluoxetine, paroxetine
Clinical uses: generalized anxiety, post-traumatic stress, OCD, panic, bulimia
First-line therapy for depression
Interactions: MAOI (serotonin syndrome), tricyclic antidepressants (toxicity)
CITALOPRAM
Significant improvement in anxiety symptoms
ESCITALOPRAM Most potent SSRI
FLUOXETINE
Longest half-life
Toxicity: weight loss
FLUVOXAMINE
Highest bioavailability
Clinical uses: OCD, panic disorder
Most drug interactions
PAROXETINE
Anticholinergic effects
Highest volume of distribution
Toxicity: weight gain, cardiac septal defects
SERTRALINE
Nausea
SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS
Moderately selective SERT and NET blockade serotoninergic and
noradrenergic effects
Clinical uses: major depression, generalized anxiety, neuropathies,
fibromyalgia
Interactions: MAOI, tricyclic antidepressants
DULOXETINE
Hepatotoxicity
MILNACIPRAN Highest bioavailability
Shortest t1/2
VENLAFAXINE
Weak NET inhibitor
Lowest protein binding antidepressant
Cardiotoxicity
TRICYCLIC ANTIDEPRESSANTS ("triptyline", "ipramine")
Oldest antidepressants
Mixed/variable SERT and NET blockade
Clinical uses: depression unresponsive to other antidepressants, pain
conditions, enuresis, migraine
Toxicity: anticholinergic effects, blockade (orthostatic hypotension), H1
antagonism (weight gain, sedation), discontinuation syndrome
Interactions: benztropin, diphenhydramine, antihypertensives
AMITRIPTYLINE
Prototype tricyclic antidepressant
MORE AFFINITY TO SERT
CLOMIPRAMINE
o Sexual effects
IMIPRAMINE
o Shortest t1/2
MORE AFFINITY TO NET
DESIPRAMINE, NORTRIPTYLINE
o No active metabolites
o Wide therapeutic window
5-HT2A RECEPTOR ANTAGONISTS ("zodone")
Inhibit 5-HT2A receptor
Little effect on NET, weak-moderate presynaptic blocker, modest H1
receptor antagonist
NEFAZODONE
Weak SERT and NET inhibitor
Potent CYP3A4 inhibitor
Toxicity: hepatotoxicity
Interactions: triazolam and simvastatin ( levels of both)

#PharMasaya :P

TRAZODONE

Weak selective SERT inhibitor

More bioavailable
Clinical uses: hypnosis
Toxicity: sedation, priapism
Interactions: ritonavir and ketoconazole ( trazodone)

Exception to the rule: vilazodone is classified as an SSRI.

TETRACYCLIC AND UNICYCLIC ANTIDEPRESSANTS
Least associated with sexual side effects: bupropion, mirtazapine
AMOXAPINE
NET > SERT inhibition
Shortest t1/2
Toxicity: parkinsonism
BUPROPION
NE and DA activity
Biphasic elimination
Toxicity: agitation, insomnia, anorexia, seizures
Interactions: cyclophosphamide, desipramine, MAOI
MAPROTILINE
Interactions: fluoxetine (additive anticholinergic and
antihistaminic effects)
MIRTAZAPINE
NE and 5-HT release
H1 receptor antagonist
Toxicity: sedation
MONOAMINE OXIDASE INHIBITORS
Block MAOA and MAOB
Toxicity: orthostatic hypotension, weight gain, amphetamine-like effects,
discontinuation syndrome
Interactions: SSRI (serotonin syndrome), tyramine (hypertensive crisis)
IRREVERSIBLE
PHENELZINE
NONSELECTIVE
o Toxicity: sexual side effects, sedation
INHIBITORS
TRANYLCYPROMINE
SELECTIVE MAOA
SELEGILINE
INHIBITORS
OTHERS
ISOCARBOXAZID, MOCLOBEMIDE
PSYCHOTIC DISORDERS
TYPICAL ANTIPSYCHOTICS
Primarily block D2 receptors but can also block , muscarinic, H1, and 5-HT2
Clinical uses: schizophrenia, Tourette syndrome
Toxicity: parkinsonism (2 to dopamine antagonism)
PHENOTHIAZINES
ALIPHATIC (CHLORPROMAZINE)
("azine")
o 1 = 5-HT2A > D2 > D1
o Toxicity: orthostatic hypotension, impaired
ejaculation, lens deposits
PIPERIDINES (THIORIDAZINE)
o Toxicity: cardiotoxicity, retinal deposits
PIPERAZINES (FLUPHENAZINE)
o Toxicity: risk of tardive dyskinesia
BUTYROPHENONES
HALOPERIDOL
("peridol")
o High potency among typical antipsychotics
o D2 > 1 > D4 > 5-HT2A > D1 > H1
o Toxicity: severe extrapyramidal symptoms,
cardiotoxicity (torsades)
DIBENZOXAPINES
LOXAPINE
THIOTHIXENE
THIOXANTHENE
o Less risk of tardive dyskinesia
DIHYDROINDOLONES MOLINDONE
ATYPICAL ANTIPSYCHOTICS
Clinical uses: manic phase of bipolar affective disorder
CLOZAPINE
Advantages: suicidal tendencies
Disadvantages: agranulocytosis, seizure threshold,
diabetes mellitus
High affinity to M1 anticholinergic effects
High affinity to 1 orthostatic hypotension
High affinity to 5-HT weight gain

Page 7 of 13

Baby Katzung (Finals Reviewer)

RISPERIDONE
OLANZAPINE
QUETIAPINE
ZIPRASIDONE

ARIPIPRAZOLE
MISCELLANEOUS

Shortest peak time (1-1.5 hours)

Moderate affinity to D2 extrapyramidal symptoms
Highest volume of distribution (10-20 L/kg)
High affinity to 1 and H1 sedation
Lowest affinity to M1
Highest protein binding (>99%)
Advantages: least weight gain (low affinity to 5-HT2)
Disadvantages: QT prolongation
Advantages: no hyperprolactinemia
PIMOZIDE
BIPOLAR DISORDERS

MOOD STABILIZERS
Inhibit inositol monophosphate (rate-limiting enzyme in inositol recycling)
LITHIUM
Classic mood stabilizer
Inhibits IP and glycogen synthase kinase-3
Narrow therapeutic window
Long-term risk of hypothyroidism
Clinical uses: manic phase of bipolar disorder,
schizoaffective disorder, unipolar depression
Toxicity: ECG changes, dermatologic effects (acne,
rashes), hypothyroid and hyperparathyroid state,
teratogenic effects (septal and valve defects), GIT
effects (anorexia, N/V, diarrhea), granulocytosis,
cognitive tremors, nephrogenic diabetes insipidus
CARBAMAZEPINE Monotherapeutic alternative to lithium
Prophylaxis and treatment of bipolar disorder
VALPROIC ACID
Inhibits IP and GSK-3
Anti-manic effect
Initial treatment and maintenance of bipolar disorder
GENERAL ANESTHESIA
INHALATION ANESTHETICS
Meyer-Overton principle: nonspecific interactions with lipid matrix of
neuronal membrane ion flux neuronal activity
Minimal alveolar concentration (MAC)
o MAC potency
o Minimum concentration resulting in immobility in 50% of patients even
with surgical stimulus or incision
o Additive in nature (used in balanced anesthesia)
o Elderly or CNS depressants (opioids, sedative-hypnotics) lower MAC
Factors DIRECTLY related to uptake
o Anesthetic concentration in inspired air
anesthetic concentration in gas mixture faster induction
o Pulmonary ventilation
Hyperventilation uptake
Factors INVERSELY related to uptake
o Solubility
Index: blood-gas partition coefficient
Low solubility or blood-gas partition coefficient rapid onset
and recovery
o Pulmonary blood flow
pulmonary blood flow faster induction of anesthesia
o Arteriovenous concentration gradient
AV gradient faster equilibration
Route of elimination: lungs (primary), liver
Toxicity: hepatotoxicity, nephrotoxicity, malignant hyperthermia
LOW-SOLUBILITY NITROUS OXIDE
o Least potent inhaled anesthetic (MAC: 100%)
o Lowest brain-blood partition coefficient (1.1)
o Not metabolized
DESFLURANE
o Highest blood-gas partition coefficient (0.42)
o Brain-blood partition coefficient: 1.3
o MAC: 6-7%

#PharMasaya :P

HALOTHANE

OTHERS

o Least metabolized among fluranes

High-solubility
Oxidized to trifluoroacetic acid and chlorotrifluoroethyl free radical halothane-induced hepatitis
SEVOFLURANE, ENFLURANE, METHOXYFLURANE
o Metabolized to fluoride ions nephrotoxicity

INTRAVENOUS ANESTHETICS
Clinical uses: rapid induction of general anesthesia, ICU sedation,
maintenance of anesthesia
Organ level effects: cerebral vasoconstriction CBF and ICP, CMRO2,
cardiorespiratory depression
BARBITURATES
THIOPENTAL, METHOHEXITAL
PROPOFOL
Potentiates Cl- current mediated through GABAA
receptor complex
Relatively short context-sensitive t1/2 even with
prolonged infusion up to 8 hours
DOC for induction and maintenance of anesthesia
BENZODIAZEPINES
MIDAZOLAM
o Rapid onset, short context-sensitive t1/2
o DOC for "conscious" sedation
o Preoperative medication (anxiolysis,
anterograde amnesia)
ANALGESICS
KETAMINE
o Blocks glutamate effects on NMDA receptor
o Lowest protein binding among IV anesthetics
o Clinical uses: dissociative anesthesia (eyes
wide open with slow nystagmic gaze)
o Causes psychotomimetic effects (emergence
reactions: vivid dreams, hallucinations)
o Minimal respiratory depression
FENTANYL
o Opioid analgesic
o Clinical uses: neurolept anesthesia (combined
with droperidol and nitrous oxide)
o Toxicity: chest wall rigidity
ETOMIDATE
GABA potentiator
Short context-sensitive t1/2
Minimal hemodynamic effects
Toxicity: adrenocortical suppression (inhibits 11hydroxylase)
DEXMEDETOMIDINE Highly-selective 2 agonist
Stimulates 2 receptors in locus ceruleus
hypnosis
LOCAL AND REGIONAL ANESTHESIA
LOCAL ANESTHETICS
Goal: localized analgesia
Block voltage-gated Na+ channels (in active or inactive state but not in
rested state) but can also act on other ion channels (K+, Ca2+), enzymes, and
receptors (NMDA, G protein, 5-HT3, NK1)
Structure: lipophilic (aromatic) ring + intermediate chain (ester or amide) +
ionizable group (tertiary amine)
Non-ionized (non-protonated) form: biologically active form
Routes: parenteral, topical (transdermal, transmucosal)
Pharmacokinetics
o More vascular site rapid absorption
o Vasoconstrictors (epinephrine) blood flow less systemic
absorption and toxic effects, better uptake
o Smaller and more lipophilic local anesthetics faster interaction
o Metabolism: plasma butyrylcholinesterase (esters), hepatic amidase
(amides)
Factors affecting local block
o Preferential blockade of small-diameter fibers (type B and C),
myelinated fast-firing fibers (type C) over large-diameter (type A) or
motor fibers

Page 8 of 13

Baby Katzung (Finals Reviewer)

o Motor fibers blocked first in large mixed nerve trunks

o Sensory fibers blocked first in extremities
Clinical uses: local infiltration, blockade of peripheral nerves, regional
anesthesia (Bier block, short surgical procedures)
Toxicity: CNS effects (dizziness, sensory disturbances, nystagmus),
neurotoxicity, tachyphylaxis, allergic reaction (2 to PABA from esters)
AMINOESTERS
COCAINE
(one i)
o First local anesthetic
o Restricted to topical anesthesia of EENT
o Vasoconstrictory property bleeding
o Toxicity: adrenergic effects from NET blockade
(vasoconstriction, hypertension, arrhythmia)
BENZOCAINE
CHLOROPROCAINE
AMINOAMIDES
ARTICAINE
(two I's)
o Dental anesthetic
BUPIVACAINE
o DOC for regional spinal anesthesia, also used in
epidural infusions for labor analgesia and postoperative pain control
o Toxicity: cardiotoxicity (antidote: lipid emulsion)
LIDOCAINE
o Intermediate-acting anesthetic
o Reference standard agent of local anesthetics
o Toxicity: transient neurologic syndrome (sudden
transient pain or dysthesia)
PRILOCAINE
o Spinal anesthetic
o Highest clearance systemic toxicity
o Metabolized to o-toluidine methemoglobinemia
ROPIVACAINE
o Same clinical uses as bupivacaine but less
cardiotoxic

MARINE
TOXINS
OTHERS

BIOLOGIC TOXINS
TETRODOTOXIN (puffer fish), SAXITOXIN (dinoflagellates)
o Bind externally to "ready" state of Na+ channels
conduction
BATRACHOTOXIN (frogs), CIGUATOXIN (moray eel)
o Bind internally to receptors in Na+ channel Na+ influx
persistent depolarization
SKELETAL MUSCLE RELAXANTS

NONDEPOLARIZING NEUROMUSCULAR BLOCKERS

Reversed by acetylcholinesterase inhibitors (neostigmine, pyridostigmine)
ISOQUINOLINE d-TUBOCURARINE
DERIVATIVES
o Prototype neuromuscular blocker
("curium")
o Paralyzes small muscles before large muscles
(abdominal, paraspinous, diaphragm)
ATRACURIUM, CISATRACURIUM
o Spontaneous chemodegradation (Hofmann
elimination) into laudanosine and quarternary acid
MIVACURIUM
o Shortest-acting nondepolarizing blocker
o Competitively inhibits acetylcholine at NM receptor
o Blocks prejunctional Na+ channels
o Rapidly cleared by plasma cholinesterase
STEROID
PANCURONIUM
DERIVATIVES
o Long-acting
("curonium")
o Most potent nondepolarizing blocker
INTERMEDIATE-ACTING (ROCURONIUM, VECURONIUM)
o ROCURONIUM: fastest-onset nondepolarizing
blocker (60-120 seconds), reversed by sugammadex

#PharMasaya :P

DEPOLARIZING NEUROMUSCULAR BLOCKERS

SUXAMETHONIUM
2 acetylcholine molecules linked together
(SUCCINYLCHOLINE) Extremely short duration of action (5-10 minutes)
Hydrolyzed by plasma cholinesterase
Pharmacodynamics
o Phase I block: fasciculation and flaccid
paralysis, augmented by cholinesterase
inhibitors
o Early phase II block: desensitization
o Late phase II block: reversed by cholinesterase
inhibitors
DOC for procedures requiring short-term
relaxation (intubation, electroconvulsive therapy)
Toxicity: malignant hyperthermia, cardiac effects,
hyperkalemia, IOP, GI regurgitation, myalgias

DIAZEPAM
BACLOFEN

TIZANIDINE

DANTROLENE

OTHERS

SPASMOLYTICS
tonic output of -motor neurons
GABA analog
Activates GABAB receptors K+ conductance
hyperpolarization presynaptic inhibition
Inhibits release of excitatory neurotransmitters in CNS and
substance P in spinal cord (analgesic effect)
2 adrenoceptor agonist (similar to clonidine but has less
antihypertensive property)
Reinforces presynaptic and postsynaptic inhibition in
spinal cord
Binds to ryanodine receptor RyR1 (in skeletal muscle)
Ca2+ release from SER
DOC for malignant hyperthermia
PROGABIDE
o GABAA and GABAB agonist
GLYCINE (endogenous inhibitory neurotransmitter)
IDROCILAMIDE, RILUZOLE
o Clinical uses: amyotrophic lateral sclerosis
BOTULINUM TOXIN
o Clinical uses: ophthalmology, relief of local spasm,
aging-associated wrinkles, generalized spasm of
cerebral palsy
ANALGESIA AND INFLAMMATION

OPIOIDS
Organ level effects: analgesia (, , ), euphoria (), sedation and
respiratory depression (), cough suppression, miosis, truncal rigidity, N/V,
hyperthermia () or hypothermia (), bradycardia (except in meperidine),
hypotension, constipation, urinary retention, peripheral effects (prolonged
labor, neuroendocrine effects, pruritus, lymphocyte proliferation)
ENDOGENOUS
ENDORPHINS ( AGONISTS)
PEPTIDES
o Precursor: preproopiomelanocortin (POMC)
o Present in CNS
o Pain modulation
ENKEPHALINS ( AGONISTS)
o Precursor: preproenkephalin (PPE-A)
DYNORPHINS ( AGONISTS)
o Precursor: leucine-enkephalin (PPE-B)
o DYNORPHIN A: found in dorsal horn
OPIOID AGONISTS
Primarily act on the opioid receptor
Chemical classifications
o PHENANTHRENES ("phine", "codeine", "codone"): morphine, codeine,
nalbuphine, buprenorphine
o PHENYLHEPTYLAMINES: methadone, propoxyphene
o PHENYLPIPERIDINES: meperidine, fentanyl, diphenoxylate, loperamide
o MORPHINANS ("orphanol"): levorphanol, butorphanol
o BENZOMORPHANS: pentazocine

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Baby Katzung (Finals Reviewer)

o MISCELLANEOUS ("adol"): tramadol, tapentadol

Routes: rectal suppositories, transdermal, intranasal, transmucosal,
parenteral (patient-controlled analgesia)
Clinical uses: analgesia, acute pulmonary edema, cough, diarrhea,
shivering, preoperative anesthesia
Toxicity: tolerance (2 to repeated doses), dependence (2 to withdrawal),
hyperalgesia (2 to persistent opioid administration)
Interactions: sedative-hypnotics (CNS and respiratory depression),
antipsychotics (sedation), MAOI (hyperpyrexic coma)
STRONG
MORPHINE
AGONISTS
o Clinical uses: moderate to severe pain
MEPERIDINE
o Only opioid analgesic with antimuscarinic activity
tachycardia
METHADONE
o Blocks NMDA receptors and monoaminergic uptake
transporters (DAT, NET, SERT)
o Clinical uses: difficult-to-treat pain (neuropathic or
cancer pain)
o DOC for opioid dependence
o Detoxification of opioids and heroin
FENTANYL
o SUFENTANIL: more potent
o ALFENTANIL: less potent, rapid-onset, short-acting
o REMIFENTANIL: short t1/2
MILD TO
CODEINE, OXYCODONE, DIHYDROCODEINE,
MODERATE
HYDROCODONE
AGONISTS
o Combined in formulations containing aspirin,
acetaminophen, and others
DIPHENOXYLATE, LOPERAMIDE
PARTIAL
NALBUPHINE
OPIOID
o Strong agonist
AGONISTSo antagonist
ANTAGONISTS BUPRENORPHINE
o High affinity but low intrinsic activity at receptor
o antagonist
o Binds to orphanin receptor ORL1
o Alternative to methadone for detoxification and
maintenance of opioid and heroin abuse
PENTAZOCIN
ANTITUSSIVES DEXTROMETHORPHAN
o Levorphanol derivative
o Strong opioid agonist
LEVOPROPOXYPHENE
OTHERS
TRAMADOL
o Centrally-acting analgesic (SERT blockade)
o Weak agonist
o Toxicity: seizures, nausea, dizziness
TAPENTADOL
o Modest affinity to receptor
o Significant NET blockade
OPIOID ANTAGONISTS
Morphine derivatives with bulkier substituent at N17 position
Reverses opioid effects within 1-3 minutes
Inert, no tolerance or withdrawal
Toxicity: abstinence syndrome
NALOXONE
Short-acting (1-2 hours)
Clinical uses: acute opioid overdose
NALTREXONE
Blocks effects of injected heroin
Maintenance of addiction
NALMEFENE
Parenteral naltrexone derivative
METHYLNALTREXONE Opioid-induced constipation
ALVIMOPAN
Post-bowel resection ileus

#PharMasaya :P

LIDOCAINE,
MEXILETINE
GABA
ANALOGS
ZICONOTIDE

NOVEL ANALGESICS
Block tetrodotoxin-resistant voltage-gated Na+ channels
GABAPENTIN, PREGABALIN
Blocks voltage-gated N-type Ca2+ channels

NONSTEROIDAL ANTI-INFLAMMATORY DRUGS

sensitivity of blood vessels to bradykinin and histamine, lymphokines,
reverse vasodilation, inhibit platelet aggregation
Newer NSAID
o Anti-inflammatory, antipyretic, analgesic
o Less GI irritation
Pharmacokinetics: enterohepatic circulation, renal elimination
Found in synovial fluid
Toxicity: tinnitus, abdominal pain, GI ulcers, hepatotoxicity (abnormal liver
function tests), asthma, pruritus, nephrotoxicity (renal insufficiency)
Greatest toxicity: indomethacin, tolmetin
Least toxicity: salicylates, ibuprofen
NONSELECTIVE ACETYLSALICYLATE (ASPIRIN)
COX
o Irreversibly inhibits COX inhibits platelet
INHIBITORS
aggregation
o incidence in TIA, unstable angina, coronary
thrombosis with MI or post-CABG
o Valuable in preeclampsia-eclampsia
o Toxicity: Reye's syndrome in children (fatal
fulminant hepatitis with cerebral edema)
NON-ACETYLATED SALICYLATES (MAGNESIUM AND
SODIUM SALICYLATE, SALICYL SALICYLATE)
o Alternative to aspirin if with renal insufficiency
SELECTIVE
CELECOXIB
COX-2
o Alternative to aspirin in patients with high risk of GI
INHIBITORS
bleeding
("coxib")
o Interactions: sulfonamides (rashes)
ROFECOXIB, VALDECOXIB
o Withdrawn due to CV thrombotic events
MELOXICAM
o "Preferentially" selective but not highly selective
COX-2 inhibitor
NIMESULIDE
o Relatively selective COX-2 inhibitor
o Analgesic and antipyretic properties
OTHERS (ETORICOXIB, PARECOXIB)
NONSELECTIVE DIFLUNISAL
NSAIDS
o No CNS entry (no antipyretic effect)
o Clinical uses: rheumatoid arthritis, cancer pain with
bone mets, pain post-third molar surgery
FLURBIPROFEN
o Clinical uses: EENT (inhibits intraoperative miosis,
perioperative analgesia in minor ear, nose, and
neck surgeries)
o Toxicity: cogwheel rigidity
IBUPROFEN (PHENYLPROPIONIC ACID)
o DOC for closure of patent ductus arteriosus in
preterm infants
INDOMETHACIN
o Inhibits phospholipase A and C
o neutrophil migration and lymphocyte
proliferation
o Clinical uses: patent ductus arteriosus closure,
initial treatment of gout, ankylosing spondylitis,
ophthalmic uses, postlaminectomy syndrome
o Toxicity: pancreatitis
KETOPROFEN
o Cyclooxygenase and lipooxygenase inhibitor
KETOROLAC
o Substitute to morphine in mild to moderate post-

Page 10 of 13

Baby Katzung (Finals Reviewer)

operative pain
o opioid requirement
MEFENAMIC ACID
o Relief of mild-moderate pain in patients 14 y/o
o Clinical uses: primary dysmenorrhea, menorrhagia
o Contraindications: status post-CABG, GI ulcers,
renal disease
NABUMETONE
o Lone nonacid NSAID
NAPROXEN
o DOC for tumor fever
PHENACETIN
o Withdrawn due to nephrotoxicity (acute tubular
necrosis, papilary necrosis)
PHENYLBUTAZONE
o Withdrawn due to aplastic anemia and
agranulocytosis
PIROXICAM
o Inhibits PMNL migration and lymphocyte function
o oxygen radicals
SULINDAC
o Clinical uses: rheumatic disease, familial
adenomatous polyposis, risk of cancer
o Toxicity: Stevens-Johnson syndrome, toxic
epidermal necrolysis
TOLMETIN
o Ineffective in gout
OTHERS (DICLOFENAC, ETODOLAC, OXAPROZIN)

DISEASE-MODIFYING ANTI-RHEUMATIC DRUGS

METHOTREXATE
Inhibits aminoimidazole carboxamide (AICAR)
transformylase and thymidylate synthetase
First-line therapy for rheumatoid arthritis
Clinical uses: arthritis, psoriasis, ankylosing
spondylitis, polymyositis, dermatomyositis,
Wegener's granulomatosis, giant cell arteritis,
SLE, vasculitis
Toxicity: nausea, mucosal ulcers
GOLD SALTS
AURANOFIN, AUROTHIOGLUCOSE
o Inhibits Schwartzmann phenomenon
IMMUNOSUPPRESANTS AZATHIOPRINE
CHLOROQUINE
CYCLOPHOSPHAMIDE
CYCLOSPORINE
LEFLUNOMIDE
MYCOPHENOLATE MOFETIL
SULFASALAZINE
o IgA and IgM rheumatoid factors
GLUCOCORTICOIDS
Management of extra-articular manifestations
of rheumatoid arthritis (pericarditis, eye
involvement, exacerbation)
Clinical uses: SLE, vasculitis, giant cell arteritis,
Wegener's granulomatosis, sarcoidosis, gout
ANALGESICS
ACETAMINOPHEN
o Phenacetin derivative
o Weak nonselective COX inhibitor
o No significant anti-inflammatory activity
o Metabolized to N-acetyl-p-benzoquinone
(hepatotoxic and nephrotoxic)
o Clinical uses: mild analgesia
o Toxicity: Reye's syndrome, severe
hepatotoxicity with centrilobular necrosis
(>15 g paracetamol)
o Antidote: N-acetylcysteine

BIOLOGICAL ANTI-RHEUMATIC DRUGS

Toxicity: risk of bacterial infections (e.g. pulmonary tuberculosis) and
lymphomas
ANTI-TNF
ADALIMUMAB
o Effective as monotherapy or in combination with
methotrexate and other DMARD
INFLIXIMAB
o Concurrent therapy with methotrexate
o Contraindications: multiple sclerosis
ETANERCEPT
o Monotherapy
o Clinical uses: rheumatoid arthritis
o risk of latent TB activation than other anti-TNF
OTHERS
ABATACEPT
o Inhibits T cell activation
RITUXIMAB
o Anti-CD20
o Combined with methotrexate
o Clinical uses: rheumatoid arthritis refractory to anti-TNF
o Toxicity: infusion reactions (pre-treat with IV
glucocorticoids)
TOCILIZUMAB
o Anti-IL-6
o Moderate to severe rheumatoid arthritis
o Same clinical uses as rituximab

COLCHICINE

ANALGESICS

URICOSURIC
AGENTS

ALLOPURINOL

FEBUXOSTAT

PEGLOTICASE

GLUCOCORTICOIDS
IL-1 INHIBITORS

#PharMasaya :P

ANTI-GOUT
Binds to intracellular protein tubulin microtubule
polymerization
Clinical uses: relief of pain and inflammation of gouty
arthritis in 12-24 hours, prophylaxis of recurrent
episodes of gouty arthritis
Overdose: burning throat pain, bloody diarrhea
Inhibit prostaglandin synthase and urate crystal
phagocytosis
INDOMETHACIN
OXAPROZIN
o Very long t1/2 (50-60 hours)
o renal excretion of uric acid
o Contraindications: renal stones
PROBENECID, SULFINPYRAZONE
o Organic acids
o Act at anion transport sites of renal tubules
o urate pool size
o Reabsorbs tophaceous urate deposits
o Clinical uses: tophaceous gout, increasingly
frequent gouty attacks
o Toxicity: GI irritation (in sulfinpyrazone),
nephrotic syndrome (in probenecid), aplastic
anemia (in both)
Isomer of hypoxanthine
Purine inhibitor of xanthine oxidase uric acid
Combined with colchicine or NSAID
Clinical uses: long-term or lifelong treatment
DOC for intercritical period (between acute attacks)
Toxicity: N/V, diarrhea, allergic reaction
Interactions: mercaptopurine, probenecid
Nonpurine inhibitor of xanthine oxidase
Clinical uses: chronic gout, prophylaxis of gout flares
(combined with colchicine or NSAID pre-therapy)
Recombinant mammalian uricase
Converts uric acid to allantoin
Clinical uses: refractory chronic gout
Clinical uses: severe symptomatic gout
ANAKINRA, CANAKINUMAB, RILONACEPT

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Baby Katzung (Finals Reviewer)

TRADITIONAL MEDICINES
Echinacea
purpurea

Ginkgo
biloba

Hypericum
perforatum

Serenoa
repens,
Sabal
serrulata

BOTANICALS
Constituents: flavonoids, water-soluble polysaccharides and
conjugates
Uses: immunomodulatory (colds, respiratory infections),
anti-inflammatory, antimicrobial
Toxicity: flu-like symptoms, unpleasant taste, GIT upset
Interactions: immunodeficiency disorders, tuberculosis,
alcohol-based medications (disulfiram-like reaction)
Constituents: flavone glycosides, terpenoids
Pharmacologic effects: vascular effects ( blood flow,
blood viscosity, vasodilation), antioxidant, CNS effects
(dementia of Alzheimer type)
Miscellaneous uses: bronchoconstriction, short-term
memory, erectile dysfunction, hearing disturbances, macular
degeneration
St. John's wort
Constituents: hypericin
Uses: antidepressant, antiviral, anticarcinogenic
Toxicity: photosensitization, mania
Interactions: antidepressants
Saw palmetto
Constituents: phytosterol, aliphatic alcohols, polyprenic
compounds, flavonoids
Uses: benign prostatic hyperplasia
Toxicity: GIT upset, hypertension, libido, abdominal pain,
back pain, urinary retention, headache
No drug interaction reported

COENZYME Q10

GLUCOSAMINE

MELATONIN

GLUTATHIONE

PAPAYA SEEDS

PURIFIED NUTRITIONAL SUPPLEMENTS

CoQ, CoQ10, uboquinone
Potent antioxidant found in mitochondria
Clinical uses: cardiovascular diseases (hypertension,
heart failure, ischemic heart disease), prevention of
statin-induced myopathy
Interactions: warfarin (CoQ10: similar to vitamin K)
Derived from crustaceans (e.g. crabs)
Substrate for articular cartilage production
Facilitates glycosaminoglycans (GAG) synthesis
Clinical uses: knee osteoarthritis
Interactions: warfarin ( INR and bleeding)
N-acetyl-5-methoxytryptamine (serotonin derivative)
Produced by the pineal gland (suppressed in daylight)
Regulates sleep-wake cycle
Inhibits reproductive function ( ovulation in females
and sperm quality in males)
Clinical uses: jetlag, insomnia
Toxicity: day-after drowsiness, fatigue, dizziness,
headache, irritability
Interactions: nifedipine ( BP)
Major endogenous antioxidant
Neutralizes free radicals and reactive oxygen species
Maintains exogenous antioxidants (vitamin C and E) in
their reduced (active) forms
Clinical uses: prevents toxic effects of chemotherapy,
aging, alcoholism, cancer, heart and liver disease,
Alzheimer's and Parkinson's disease
Toxicity: rashes, stomachache, thyroid disease, fatal
effects (renal failure, SJS, toxic epidermal necrolysis)
Contraindications: allergy to milk protein, organ
transplant
Uses: anti-inflammatory, anti-parasitic (ringworm
infections), analgesic (stomachache)
Toxicity: allergic reaction (skin irritation)

#PharMasaya :P

AKAPULKO
(Cassia alata)

AMPALAYA
(Momordica
charantia)
ATIS (Anona
squamosa)

BANABA
(Lagerstromia
speciosa)
BAWANG (Allium
sativum)

BAYABAS
(Psidium
guajava)
GUMAMELA
(Hibiscus rosasinensis)

LAGUNDI (Vitex
negundo)

LUYA (Zingiber
officinale)

MABOLO
(Diospyros
blancoi)
MALUNGGAY
(Moringa
oleifera)

MAKABUHAY
(Tinospora
rumphii Boerl)
NIYOG-NIYOGAN
(Quisqualis
indica)
OREGANO
(Origanum
vulgare)

PANDAN
(Pandanus
tectorius)
PANSITPANSITAN
(Peperomia
pellucida)

HERBAL MEDICINES
Constituents: saponins (laxative)
Uses: antifungal, ringworms, scabies, eczema,
stomatitis, expectorant, anti-asthma, diuretic, laxative
Toxicity: GIT effects (N/V, diarrhea)
Constituents: flavonoids, alkaloids (antihyperglycemic)
Uses: antihyperglycemic, antirheumatic, antiseptic,
antihelminthic, immunomodulatory
Toxicity: abortifacient
Uses: gastrointestinal (dysentery, diarrhea), colds,
fever, antirheumatic, dizziness and fainting,
antipediculosis
Toxicity: blindness (seeds), abortion (paste)
Queen's flower, crepe myrtle
Constituents: corosolic acid (insulin-like effect)
Uses: antihyperglycemic, obesity, blood pressure
Cautions: antidiabetics
Constituents: alliin
Uses: antihypertensive, antifungal, fibrinolytic
Toxicity: nausea, hypotension, allergy, bleeding
Cautions: anticoagulants
Uses: wound disinfectant, antiseptic gargle,
astringent, vaginal wash
China rose or hibiscus
Uses: expectorant, diuretic, emollient, anti-infective
and anti-inflammatory (boils, swelling, abscesses,
mumps), antipyretic, sedative
Toxicity: abortifacient in large doses
Constituents: chrysoplenol D (antihistamine, muscle
relaxant)
Uses: respiratory uses (asthma, pharyngitis, cough,
colds, flu, bronchopulmonary disorders), boils,
symptomatic management of chicken pox,
antihelminthic
Uses: analgesic (rheumatic and muscle pain,
toothache), alleviates sore throat and colds, GI uses
(tympanism, flatulence, intestinal worms, diarrhea, gas
pains, dyspepsia), serum cholesterol, PTB treatment
Contraindications: pregnancy (testosterone inhibition)
Uses: gastrointestinal uses (stomach pains, diarrhea,
dysentery), cardiovascular uses (heart disease,
hypertension), cough, fever, skin ailments, diabetes
Horse radish
Uses: nutrient supplement (source of Ca2+, iron,
vitamin C, phosphorus), antioxidant, antidiabetic,
antihypertensive, analgesic (rheumatic pain, headache,
migraine), purgative, antifungal
Heavenly elixir
Uses: antimalarial, wound cleansing, diarrhea,
indigestion, scabies
Chinese honey suckle
Uses: antiparasitic
Winter marjoram
Constituents: antioxidants
Uses: respiratory uses (cough, colds, asthma), antiaging, arthritis, GI uses (upset stomach, dyspepsia,
indigestion), UTI, dermal uses (heals wounds, insect
bites or stings)
Fragrant screw pine
Uses: analgesic, antiseptic and antibacterial
Ulasimang-bato
Uses: arthritis, gout, skin diseases (boils, abscesses,
acne), headache, abdominal pain, kidney problems

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Baby Katzung (Finals Reviewer)

SABILA OR ALOE
VERA
(Barbadensis
miller)
SALUYOT
(Corchorus
capsularis)
SAMBONG
(Blumea
balsamifera)
SILYMARINE OR
MILK THISTLE
(Silybum
marianum)

TANGLAD
(Andropogon
citratus DC)
TSAANG- GUBAT
(Ehretia
microphylla)
YERBA BUENA
(Mentha
cardifolia)

Uses: skin conditions (acne, psoriasis, bites, minor

burns), analgesic, antihypertensive, anti-aging,
diabetes, eradicates intestinal bacteria and parasites,
helps prevent cancer and tumors
Constituents: Ca2+, phosphorus, iron, K+, vitamin A,
thiamine, riboflavin, ascorbic acid, fibers
Uses: antioxidant, reduce wrinkles, anti-inflammatory
Uses: diuretic, kidney stones, hypertension,
rheumatism, colds, fever, GI uses (diarrhea, stomach
pains, dysentery), worms, boils, sore throat
Toxicity: hypokalemia (take with bananas or potatoes)
Constituents: silymarin (polyphenolic flavonoid with
antioxidant properties)
Uses: hepatoprotection (improves liver function in
cirrhosis and chronic hepatitis), Amanita phalloides
poisoning, antidiabetic, anticholesterol, reduces
growth of cancer cells (breast, prostate, cervix, skin),
antioxidant
Nontoxic (no overdose symptoms)
Lemon grass
Uses: cleansing, stomach discomfort, antibacterial and
antifungal, antiuricemic, detoxifier
Forest or wild tea
Uses: GI uses (gastroenteritis, intestinal motility,
dysentery, diarrhea or LBM, mouth gargle), body wash
Uses: analgesic (headache, stomachache, rheumatic or
arthritic pain, menstrual and gas pains), dental uses
(swollen gums, toothache), nausea, fainting, pruritus

PHARMACOLOGY TRANSCRIPTION TEAM

Martin Joseph A. Calaunan @MARTINidazole
Transmaster/Editor
Nikka Mae A. Larcia @NIKKArdipine
Nina Carmela P. Pescante @PESKYcide
Marc Christopher F. Barbin @phenoBARBital
Clarice B. Palma @CLArithromycin
Ron Michael N. Olaguera @interfeRON

#PharMasaya :P

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