Professional Documents
Culture Documents
Drug
Antiepileptic:
Seizures:
Anticonvulsants
Carbamazepine
(drug of choice in
Parial
and tonic cloinc
seizures)
Phenytoin
Phosphenytoin
Oxcarbamazepine
Clonazepam
Ethosuximide (drug
of choice in
absence
seizures)
Felbamate
Gabapentin
Lamotrigine
Phenobarbital (drug
of choice of febrile
seizures and grand
mal seizures in
children)
Primidone
Tiagabine
Topimarate
Valproate
Sodium divalproex
Vigabatrin
Levetiractem
Mechanism of action
Many typical anticonvulsants
work by blocking
voltagesensitive sodium
channels in the brain.
Phenobarbital potentiates synaptic
inhibition through an action on
GABA receptor.
Ethosuximide inhibits calcium ion
influx through T type channels in
the thalmic neurons.
Gabapentin promotes the release of
GABA.
Absence seizures (sometimes
referred to as petit mal seizures)
involve an interruption to
consciousness where the person
experiencing the seizure seems to
become vacant and unresponsive
for a short period of time (usually
up to 30 seconds).
Slight muscle twitching may occur.
Tonic-clonic seizures (sometimes
referred to as grand mal seizures),
involve an initial contraction of the
muscles (tonic phase) which may
involve tongue biting, urinary
incontinence and the absence of
breathing.
Myoclonic seizures involve
sporadic muscle contraction and
can result in jerky movements of
muscles or muscle groups.
Atonic seizures involve the loss of
muscle tone, causing the person to
fall to the ground. These are
sometimes called 'drop attacks' but
should be distinguished from
similar looking attacks that may
occur in narcolepsy or cataplexy.
Side effect
Carbamazepine: NV,
Jaundice, abdominal pain, pale
stool, darkened urine, unusual
bruising bleeding, fever, sore
throat, ulcer in the mouth,
dizziness, drowsiness,
unsteadiness.
Phenytoin: NV, swollen
gums, rash, swollen glands,
bleeding, jaundice, fever, sore
throat.
Phosphenytoin: Similar to
phenytoin.
Oxcarbazepine: NV,
dermatological reactions,
dizziness, somnolence,
headache, ataxia, fatigue,
cognitive symptoms, vertigo,
abdominal pain, abnormal
gait, tremor, diplopia,
nystagmus, abnormal vision.
Hyponatremia.
Clonazepam drowsiness,
ataxia, behavior disturbances
in children, hypersalivation,
bronchial hypersecretion,
anemia, leukopenia,
thrombocytopenia, respiratory
depression, anorexia, weight
loss.
Ethosuximide NV, fatigue,
headaches, drowsiness,
eosinophilia,
granulocytopenia, leukopenia,
blurred vision, hiccups,
confusion, urticaria, SSS, renal
damage, periorbital edema.
Felbamate: N, infection,
aplastic anemia, liver failure,
acne, insomnia, headache,
anxiety, hyperactivity, fatigue,
Interaction
Carbamazepine
Antiepileptic drugs,
antibiotics, isoniazid,
cimetidine,
propoxyphene,
diltiazem, verapamil,
CCB, warfarin, TCAs
and grapefruit juice.
Phenytoin
Antiepileptic drugs,
disulfiram, isoniazid,
chloramphenicol,
propoxyphene,
corticosteroids,
digitoxin, doxycycline,
estrogens, furosemide,
oral contraceptives,
quinidine, rifampin,
theophylline, vit D,
enteral nutritional
therapy, coumarin,
warfarin, TCAs,DM,
arthritis drugs.
Phosphenytoin
Amiodarone, quinidine.
Oxcarbazepine:
Phenytoin
phenobarbital, oral
contraceptive.
Clonazepam
Phenytoin, levodopa,
digoxin.
Ethosuximide
Carbamazepine,
valproic acid.
Felbamate:
Phenytoin,
carbamazepine.
Valproic acid.
Gabapentin Antacids,
cimetidine, oral
Contraindications:
Carbamazepine: CBC should be
monitored; can lower white blood
cell count.
Therapeutic drug monitoring is
required Caution: in patients with
bone marrow depression,
glaucoma and elderly.
REM dermatological reactions,
blood dyscrasias, suicidal thoughts
and behavior.
PhenytoinMyocardial insufficiency
hypotension, renal failure and
elderly.
Clonazepam
Caution: Patients with psychoses,
acute narrow-angle glaucoma, and
significant liver disease.
REM: withdrawal symptoms with
abrupt discontinuation, suicidal
thoughts and behavior.
Ethosuximide Avoid exposure to
sunlight and ultraviolet light and
alcoholic beverages
REM: Blood dyscrasias, systemic
lupus erythematosus, suicidal
thoughts and behavior. Hepatic
and renal toxicity.
Gabapentin
REM: Suicidal thoughts and
behavior.
Lamotrigine: Caution: in renal,
hepatic, or cardiac impairment.
Phenobarbital:
Caution in patients with hepatic
disease and elderly
Tiagabine:
To monitor: Periodic
ophthalmological. REM: Suicidal
thoughts, behavior.
Topimarate:
REM: Suicidal thoughts, behavior,
peripheral edema,
vasodilation, hypotension,
HTN, diplopia blurred vision,
anorexia, weight decrease, QT
prolongation and torsade de
pointes.
Gabapentin Somnolence,
dizziness, ataxia, nystagmus,
dyspepsia, dryness of mouth,
constipation, increased
appetite, diplopia, blurred
vision, CHF, HTN /
hypotension, dry skin, fungal
dermatitis, herpes infection,
SSS, DM.
Lamotrigine:
NV, dizziness, diplopia, ataxia,
blurred vision, rash, SSS,
photosensitization.
Phenobarbital: NV,
respiratory depression,
Withdrawal convulsions.
Tiagabine: Confusion,
dizziness, fatigue, GI upset,
mouth ulceration, and
anorexia, EEG abnormalities,
sudden unexpected death,
rash.
Topimarate: N, breast pain in
females, tremor, back pain,
chest pain, dyspepsia, leg
pain.
Valproic acid: NV, abdominal
pain, anoxia.
Vigabatrin:
Somnolence, fatigue, lightheadedness, peripheral
neuropathy, anemia,
depression.
Levetiracetam: Somnolence,
weakness, hostility, infection,
dizziness, depression,
nervousness, pruritis, skin
discoloration, rash, alopecia,
contraceptives.
Lamotrigine:
Carbamazepine,
phenobarbital,
primidone, valproic
acid.
Phenobarbital:
Antiepileptic drugs,
acetazolamide,
chloramphenicol,
cimetidine,
furosemide, rifampin,
pyridoxine, ethanol.
Tiagabine:
Phenobarbital,
phenytoin,
carbamazepine. Take
with food.
Topimarate:
Phenytoin,
carbamazepine.
Valproic acid:
Antiepileptic drugs,
aspirin, warfarin,
antacids.
teratogenic effects.
Vigabatrin: REM: Vision loss,
suicidal thoughts and behavior.
Antidepressants:
SSRIs
Fluoxetine (Prozac;
Sarafem)
Sertraline (Zoloft)
Escitalopram:
(Lexapro:Cipralex)
Citalopram(Celexa)
Fluvoxamine (Luvox)
Paroxetine (Paxil)
Selective
Norepinehprine
Reuptake
Inhibitor (SNRI)
Venlafaxine (effexor)
TCAs;
Antidepressants
amitriptyline (Elavil)
amoxapine (Asendin)
clomipramine
(Anafranil)
desipramine
(Norpramin)
doxepin (Adapin,
Sinequan)
imipramine (Tofranil)
nortriptyline
(Pamelor)
trimipramine
(Surmontil)
Tetracyclic
Antidepressant
Remeron
(Mirtazipine)
drowsiness, cough.
Fewer and less severe than
TCAs and MAOI.
Insomnia, GI effects (nausea,
vomiting),
sexual dysfunction, a nxiety
WITHDRAWL SYMPTOMS: On
abrupt discontinuation
nightmares and vivid dreams
so tapered dose needed
Metabolised by CYP450
and CYP2D6 so drug
interactions are
common
Similar to SSRIs
Also produce withdrawal
symptoms.
Antipsychotic:
Schizophrenia
Typical
Antipsychotics
Chlorpromazine
Fluphenazine
Haloperidol
Thiothixene
Thioridazine
Trifluoperazine
Loxapine
Atypical
Antipsychotics
Clozapine (Clozaril)
Olanzapine (Zyprexa)
Quetiapine
(Seroquel)
Risperidone
(Risperidal)
DA
Schizophrenia
DA PD
Mood Stabilizers
Lithium carbonate.
Clozapine:
Complete blood count (CBC) must
be monitored.
Caution in patients at risk for
seizures or with a history of a
seizure disorder.
Increase Li levels:
ACEIs, ARAII, NSADs,
thiazides, dehydration,
Anticonvulsants:
Valproic acid,
Carbamazepine
Oxcarbazepine
Gabapentin
Lamotrigine
Topiramate
5-HT3 receptor
blockers
Antiemetic
Granisetron
Ondansetron (zofran)
Dolasetron (anzemet)
Metoclopramide (GIT
Metoclopramide is a
Alzheimers
Disease; Dementia
donepezil (Aricept)
galantamine
(Reminyl)
rivastigmine (Exelon)
Mematine (NMDA
receptor
Antagonist) A
novel drug
leukocytosis, polyuria.
Long term: Morphological
kidney changes, EKG changes,
bradycardia, weigth gain,
decreased libido,
hypothyroidism, rash, acne.
Toxicity: Severe drowsiness,
coarse hand tremor, muscle
twitching, seizures,
choreoathetosis, vomiting,
confusion, vertigo.
Confusion, agitation,
restlessness.
Headache.
Dolasetron:
Electrocardiographic changes
(prolonged QT interval).
Antidopaminergic: Sedation,
diarrhea, and extrapyramidal
renal dysfunction,
Sodium los, and
fluoxetine.
Decrease Li levels:
Acetazolamide,
methylxanthines,
osmotic diuretics,
pregnancy (3third
trimester), sodium
supplements, urine
alkalinizers.
Others: Antipsychotics,
benzodiazepines,
Are substrates for
cytochrome P450
(except Rivastigmine).
impairment, cardiovascular
disease, dehydration, seizure
disorder, and thyroid disease.
Consider: age, weight, and renal
function
motility inhibitor;
Prokinetic)
1
0
Anti Migraine; 5 HT
Receptors
Agonists
(Triptans)
Sumatriptan (Imitrex)
5HTD1
Rizatriptan (Maxalt)
Naratriptan (Amerge)
Zolmitriptan (Zomig)
5HTB1/D1
1
1
Antiarrrhythmics
Class Ia agents
include quinidine,
procainamide and
disopyramide.
Class Ib agents
include lidocaine,
mexiletine, tocainide,
and phenytoin.
Class Ic agents
include encainide,
flecainide,
moricizine, and
propafenone.
Class II agents
include esmolol,
propranolol, and
metoprolol.
Class III agents
include amiodarone,
azimilide, bretylium,
clofilium, dofetilide,
ibutilide, sematilide,
and sotalol.
parasympa-thomimetic, and is
also a potent dopamine
antagonist that enters the central
nervous system. It is used for
gastric emptying in patients with
gastric motor failure (gastroparesis).
Triptans are a family of tryptamine
drugs used in the treatment of
migraine and cluster headaches.
Their action is attributed to their
binding to serotonin 5-HT1B and 5HT1D receptors in cranial
blood vessels (causing their
constriction) and subsequent
symptoms
Monoamine oxidase
inhibitors (MAOIs):
(excluding eletriptan,
frovatriptan, and
naratriptan).
Eletriptan:
ketoconazole,
itraconazole,
nefazodone,
troleandomycin,
clarithromycin,
nelfinavir, and
ritonavir.
1
2
1
3
Class IV agents
include verapamil
and diltiazem.
Class V agents
include adenosine
and digoxin.
node.
Class V agents work by other or
unknown mechanisms.
Calcium Channel
Blockers
Dihydropyridine
calcium channel
blockers
Amlodipine besylate
(Norvasc)
Nicardipine (Cardene,
Carden SR)
Nifedipine (Procardia,
Adalat)
Nitrendipine (Cardif,
Nitrepin)
Nimodipine
(Nimotop)
Phenylalkylamine
calcium channel
blockers
Verapamil
hydrochloride (Calan)
Diltiazem
hydrochloride
(Cardizem)
Fibrates;Hyperchol
esterolemia
Clofibrate (largely
obsolete due to sideeffect
profile, e.g.
gallstones)
Gemfibrozil (e.g.
Lopid)
Fenofibrate
Bezafibrate (e.g.
Bezalip)
deposits (reversible)
Hypo or hyperthyroidism.
Photosensitivity.
Pulmonary fibrosis.
Sotalol: Arrhythmias.
Verapamil: Sinus
bradycardia.
AV block. GI upset.
Verapamil: Constipation,
hypotension, bradycardia,
edema, CHF, GI upset.
Diltiazen: Edema, headache,
dizziness, asthenia, Rash.
Nifedipine: MI, peripheral
edema, reflex tachycardia,
Headache, flushing, edema.
Fibrates:
Muscle damage when fibrate
added with statin.
Gallstone formation.
NVD.
Statins
atorvastatin
(Lipitor)
fluvastatin (Lescol)
lovastatin
(Mevacor,
Altocor, not
marketed in the UK)
pravastatin
(Pravachol,
rosuvastatin
(Crestor)
simvastatin (Zocor)
1
4
Diuretics
Osmotic diuretics
(e.g., mannitol)
Carbonic
anhydrase
inhibitors (e.g.,
acetazolamide,
dorzolamide)
Thiazides (e.g.,
hydrochlorothiazide,
bendroflumethiazide)
Osmotic Diuretics:
Headache, NV, Chills,
dizziness, polydipsia.
Carbonic Anhydrase
Inhibitors: Acidosis.
THIAZIDE DIURETICS:
Chlorothiazide: hypokalemia,
hyponatremia, hyperglycemia,
hiperuricemia,
hypercalcemia, oliguria,
anuria, decreased placental
flow.
Loop Diuretics:
Furosemide: Ototoxicity,
hypovolemia,
hypomagnesemia.
hypokalemia
Loop diuretics
(e.g., furosemide,
bumetanide,
ethacrynic acid)
Potassium-sparing
diuretics (e.g.,
spironolactone,
amiloride,
triamtrene)
1
5
Alpha Adrenergic
Receptor Blockers
Alfuzosin
Doxazosin
Terazosin
Prazosin
Tamsulosin
1
6
hyponatremia, hyperglycemia,
sulfonamide allergy.
Ethacrynic acid:Most
ototoxic.
POTASSIUM SPARING
DIURETICS:
Hyperkalemia, sodium or
water depletion, patients with
DM may develop glucose
intolerance, endocrine
disturbances. Triamterene
will turn urine blue.
1
7
Sulfonylurea;
Antidiabetic
First generation:
Chlorpropamide
Tolbutamide
Tolazamide
Second
generation:
Glipizide , Gliclazide
Glibenclamide ,
Glimepiride
Glyburide
1
8
Cancer
Alkylating Agents
Cisplatin,
Carboplatin,
Ifosfamide,
Chlorambucil,
Busulfan, Thiotepa.
Cyclophosphamide
Cancer;
Antimetabolites
5 Fluoro Uracil (5 FU)
Methotrexate,
Fludarabine
Thiazolidinediones require
insulin to be present for their
action. Thiazolidinediones exert
their principal effects by increasing
insulin sensitivity in peripheral
tissue but also may lower glucose
production by the liver.
Sulfonylureas bind to an ATPdependent K+ channel on the
cell membrane of pancreatic beta
cells. This inhibits a tonic,
hyperpolarizing outflux of
potassium, which causes the
electric potential over the
membrane to become more
positive. This depolarization opens
voltage-gated Ca2+ channels. The
rise in intracellular calcium
leads to increased fusion of
insulin granulae with the cell
membrane, and therefore increased
secretion of proinsulin.
Alkylating agents are so named
because of their ability to add
alkyl groups to many
electronegative groups
undervconditions present in
cells. They stop tumor growth
by crosslinking guanine
nucleobases in DNA doublehelix strands - directly
attacking DNA. This makes the
strands unable to uncoil and
separate.
Anti-metabolites masquerade as
purine or pyrimidine which
become the building blocks of DNA.
They prevent these
substances becoming incorporated
in to DNA during the "S"
phase (of the cell cycle),
stopping normal development and
division. An important example is 5-
Alkylating Agents
Cisplatin: Nephrotoxicity,
nausea and vomiting,
peripheral neuropathy,
myelosuppression, ototoxicity.
Carboplatin:
Myelosuppression, nausea and
vomiting, peripheral
neuropathy, ototoxicity.
Ifosfamide:
Myelosuppression,
hemorrhagic cystitis,
somnolence, confusion.
Chlorambucil:
Myelosuppression, pulmonary
fi brosis, hiperuricemia.
Busulfan:
Myelosuppression, pulmonary
fi brosis, aplastic anemia, skin
Hyperpigmentation. Thiotepa:
Myelosuppression, nausea and
vomiting, mucositis, skin
Alkylating agents:
Pregnancy, patients with bone
marrow suppression, Renal
disease(with cisplatin)
Platinum Analogs:
Hypersensitivity to
cisplatin/platinum products or
mannitol
Severe
myelosuppression/significant
bleeding
Antimetabolites:
Caner; Plant
alkaloids
Vincristine
Vinblastine
rashes. Cyclophosphamide:
Myelosuppression,
hemorrhagic cystitis,
immunosuppression, alopecia,
stomatitis, SIADH
Antimetabolites:
5 FU: Stomatitis,
myelosuppression, diarrhea,
nausea and vomiting,
cerebellar ataxia.
Methotrexate: Mucositis,
myelosuppression, pulmonary
fi brosis, hepatotoxicity,
nephrotoxicity, diarrhea, skin
erythema.
Fludarabine:
Myelosuppression, nausea and
vomiting, fever, malaise,
pulmonary infi ltrates.
Plant alkaloids:
Vincristine: Peripheral
neuropathy, paralytic ileus,
SIADH
Vinblastine: Myelosuppression,
paralytic ileus, alopecia,
nausea, stomatitis.
Antibiotics:
Daunorubicin:
Myelosuppression,
cardiotoxicity, stomatitis,
alopecia, nausea and
vomiting.
Bleomycin: Pneumonitis,
pulmonary fibrosis, fever,
anaphylaxis,
hyperpigmentation,
alopecia
Actinomycin: Bone marrow, a
cough, sore throat, pain,
passing urine or may feel cold
and shivery, anemia, bruising,
hair loss, skin changes.
Plicamycin: headache, NV,
vesicant, hepatic injury,
Ampicillin, aspirin,
Nsaids,
Cephalosporins.
Plant alkaloids:
Drugs known to inhibit
drug metabolism by
hepatic CYP 3A
subfamily. Vincristine
sulfate: Itraconazole.
Antibiotics:
Cyclophosphamide doxorubicin.
Antibiotics: Hypersensitivity,
Children < 12 years, myeloid
malignancies, heart failure, atrial
arrhythmias, thromboembolic
disorders.
Caution: Major organ dysfunction.
Plicamycin: Breast feeding.
1
9
Immunosuppressa
nt, Eczema
Organ Transplant
Tacrolimus (Prograf,
Protopic)
Mycophenolate
mofetil (Cellcept)
Cyclosporine
2
0
Immunosuppressiv
e
Azathioprine
2
1
DMARD
gold salts (sodium
aurothiomalate,
auranofin)
D-penicillamine
chloroquine and
hydroxychloroquine
(antimalarials)
Tacrolimus:
Antiepileptic drugs,
rifampin isoniazid,
azole antifungal
agents , macrolide
antibiotics,
calcium-channel
blockers, antiviral
agents
Xanthine oxidase
inhibitor, allopurinol,
sulfasalazine (SSZ)
methotrexate (MTX)
azathioprine
cyclosporin A
2
3
Antithyroids
PTU
(propylthyouracil)
Tepazole
(methimazole)
2
4
Corticosteroids
Prednisone
Leflunomide (Arava)
2
2
Proton Pump
Inhibitors (PPIs)
Omeprazole,
Lansoprazole,
Esomeprazole,
Pantoprazole,
Rabeprazole
Inhibit CYP2C19
Diazepam, warfarin,
phenytoin, clopidogrel,
theophylline
Estrogens, oral
contraceptives,
Methylprednisone
Dexamethasone
2
5
Anti obesity
Orlistat (Xenical)
2
6
OCPs
Birth Control Pills
2
7
Inflammatory
Bowel Disease
immunosuppressive
properties.They bind to
glucocorticoid
receptors altering DNA and
RNA translation causing drop in
circulating T lymphocytes. As a
consequence, corticosteroids
are widely used as drugs to treat
inflammatory conditions such as
arthritis or dermatitis, and as
adjunction therapy for
conditions such as autoimmune
diseases.
It works by inhibiting pancreatic
lipase, an enzyme that breaks
down fat in the intestine.
Without this enzyme, fat from the
diet is excreted undigested, and not
absorbed by the body.
The Pill works by preventing
ovulation, as well as making
the uterus less likely to accept
implantation of an embryo if
one is created, and thickens
the mucus in the cervix making
it more difficult for sperm to
reach any egg. Taken correctly, it
is the
single most reliable form of
reversible contraception. Most
brands use 20 to 40 micrograms of
ethinyloestradiol as the
estrogen component and either a
fixed or varying (the bi and
triphasic pills) amount of
progestogen as the
progesterone analogue. Most
progestagens are used for their
antiestrogenic properties in oral
contraceptives to avoid over
stimulation of the endometrium
which could lead to endometriosis.
Ulcerative colitis is an inflammatory
disease of the bowel, that usually
hemorrhage, ulcerative
esophagitis, acute
pancreatitis, weight gain,
osteoporosis, hyperglycemia,
acne, increased susceptibility
to infection, cushingoid moon
face, buffalo hump,
headache, vertigo, increased
intraocular, glaucoma,
cataracts intracranial
pressures, muscle weakness,
psychological disturbances,
edema, HTN.
GI (soft or liquid stools),
increased defecation, fecal
urgency, abdominal pain,
decreased absorption of
vitamins A, D, E, K, and betacarotene.
Relatively low: Most due to
estrogen component.
Cardiovascular both. Breast
fullness, depression, fluid
retention, headache, NV.
Carcinogenicity: Increased
incidence of cervical cancer,
induce other neoplasms.
Production of benign tumors,
hemorrhage, abnormal
glucose tolerance, weight gain
(nortestosterone) (less weight
gain drospirenone). Changes in
the serum lipoprotein profile.
itraconazole, macrolide
antibiotics,
cyclosporine,
potassium-depleting
diuretics, digitalis
glycosides.
Mesalamine (5 ASA):
Diarrhea, headache,
Mesalamine
Mercaptopurine,
Fish oil.
Cerebrovascular, thromboembolic
disease, estrogen dependent
neoplasms, liver disease, and
pregnancy. Age of 35 who are
heavy smokers.
(IBD)
Ulcerative Colitis and
Crohns Disease
Mesalamine (5
ASA) (Pentasa,
Asacol)
Olsalazine
olsalazine,
balsalazide
antacids or acid
lowering agents.
Sulfasalazine
Fever, dizziness, headache,
itching, rash, photosensitivity,
GI upset, nausea, vomiting,
diarrhea, reversible
oligospermia
Sulfasalazine
folic acid
Zafirlukast: Headache,
dizziness, nausea, diarrhea
Zafirlukast: Aspirin,
erythromycin,
theophylline,
terfenadine, warfarin,
dofetilide.
Sulfasalazine
2
8
Leukotriene
receptors
antagonists
(LTRA); Asthma
Zafirlukast
(Accolade)
Montelukast
(Singulair)
Montelukast: Hepatic
enzyme inducers (e.g.,
rifampin,
phenobarbital).
2
9
Bisphosphonates
Alendronate
Risedidronte
etidronate
3
0
Influenza A and B
Tamiflu (Oseltamivir)
Zanamivir
3
1
Influenza A (Flu)
Amantadine
3
2
Anticoagulants
Warfarin
Phenindione
Warfarin:
Hemorrhage, skin lesions,
necrosis, purple toe syndrome,
alopecia.
Warfarin: Numerous:
Inhibition of
metabolism: Acute
alcoholintoxication,
cimetidine,
chloramphenicol,
cotrimoxazole,
disulfiram,
metronidazole.
Stimulation : Chronic
alcohol, ingestion,
barbiturates,
glutethimide,
griseofulvin, rifampin
Antagonist: Spinach,
broccoli.
Additive effect:
Garlic.
Warfarin:
Pregnancy (X)
Black box warning for bleeding
risk.
Monitor and adjust the
anticoagulant effect.
To monitor: if necessary:
response with prothrombin
time/INR measurements.
Heparin:
Hypersensitive, bleeding disorders;
alcoholics; having or have had
recent surgery of the brain, eye,
spinal cord.
Heparin
3
3
Beta Blockers
Cardioselective
Acebutolol, Atenolol,
Betaxolol Bisoprolol,
Esmolol, Metoprolol
Nebivolol
Nonselective
Nadolol, propanolol,
Sotalol, Pindolol,
3
4
Biguanide;
Glucophage
To monitor:
The bleeding time.
Heparin: Hemorrhage,
Hypersensitivity reactions
(chills, fever, urticaria,
anaphylactic shock),
thrombosis,
thrombocytopenia,
osteoporosis, abnormal liver
function tests.
Heparin:
Protamine sulfate
(neutralization).
Propanolol:
Bronchoconstriction, sexual
impairment, disturbance in
metabolism, fasting
hypoglycemia.
Propanolol:
Cimetidine, fluoxetine,
paroxetine, ritonavir,
barbiturates,
phenytoin, rifampin
Vitamin B12,
intravenous
radiographic contrast
agents.
3
5
Digitalis: Cardiac
Glycoside
Digoxin
3
6
Selective Estrogen
Receptor
Modulator
(SERM)
clomifene (an
ovulation)
raloxifene
(osteoporosis)
tamoxifen (breast
cancer)
toremifine (breast
cancer)
3
7
Antiretroviral
Drugs; HIV
Protease inhibitors
(PIs); HIV
Saquinavir, Ritonavir,
N, headache, fatigue,
confusion, color perception
alteration, halos in dark
objects. Hypercalcemia and
hypomagnesemia. Ventricular
tachycardia.
Quinidine, verapamil,
amiodarone, K
depleting diuretics,
corticosteroids.
Clomiphene: Headach,
nausea, vasomotor flushes,
visual disturbances, ovarian
enlargement.
Toremifene: Endometrial
hyperplasia.
Raloxifene: Hot flashes, leg
cramps, deep vein thrombosis,
pulmonary embolism, retinal
vein thrombosis.
PIs:
Saquinavir: Prolongs PR and
QT interval, torsades de
pointes.
Ritonavir: GI intolerance,
PIs:
Warfarin.
Ritonavir:
inhibits many P450
isoenzymes
Indinavir, Nelfinavir
Reverse
Transcriptase
Inhibitors (RTIs)
Nucleoside Analog
Reverse
Transcriptase
Inhibitors (NARTIs) or
(NRTIs).
(Zidovudine,
didanosine,
Zalcitabine,
Stavudine,
Lamivudine,
Abacavir)
Non-Nucleoside
Reverse
Transcriptase
Inhibitors (NNRTIs)
(nevirapine:
Viramune, efavirenz:
Sustiva,
delavirdine:
Rescriptor)
circumoral paresthesias,
hyperlipidemia,
hyperglycemia, fat
maldistribution, liver
function tests, taste
perversion.
Indinavir: Nephrolithiasis,
indirect hyperbilirubinemia,
hyperglycemia,
hyperlipidemia, fat
maldistribution,
headache, GI intolerance.
Nelfinavir: D, GI intolerance,
hyperlipidemia,
hyperglycemia, fat
maldistribution, pancreatitis,
PR interval prolongation.
RTIs
Zidovudine: Bone marrow
suppression, macrocytic
anemia, neutropenia,
headache, malaise, seizures,
anxiety, fever, rash,
symptomatic myopathy.
Didanosine: Reversible
peripheral neuropathy,
pancreatitis.
Stavudine: Reversible
peripheral neuropathy,
headache, rash, NVD. Fatal
episodes of pancreatitis.
Lamivudine: Minor.
Headache, fatigue, GI
reactions (NVD), dizziness,
neuropathy, insomnia.
NNRTIs
Nevirapine: SSS, N,
symptomatic hepatitis, fever,
headache.
Efavirenz: Insomnia,
dizziness, drowsiness,
nightmares, hallucinations,
rash, transaminases, GI
disturbances.
Indinavir: Atazanavir,
Vitamin C.
Nelfinavir Methadone.
RTIs
Zidovudine:
Cotrimoxazole,
atovaquone, valproic
acid, methadone,
probenecid, cytotoxic
drugs ganciclovir,
dapsone, ribavirin,
interferonalpha,Rifabut
in, rifampin.
Didanosine:
Zalcitabine:
Stavudine:
Zidovudine.
Lamivudine:
Cotrimoxazole,
emtricitabine.
Abacavir: Alcohol
NNRTIs
Rash, hepatotoxicity.
Nevirapine:
Methadone
Efavirenz: St. Johns
wort, levonorgestrel.
Delavirdine:
Alprazolam,
midazolam, triazolam,
simvastatin, lovastatin,
rifabutin, cisapride.
PPIs and H2-receptor
antagonists, St. Johns
wort, carbamazepine,
phenobarbital,
phenytoin, rifampin.
Antituberculosis
Rifampin
Rifampin: Serious
hepatotoxicity, skin rash,
drowsiness, headache, fatigue,
confusion, NV, abdominal pain.
Colors urine, sweat, tears,
saliva, feces orange-red.
Influenza-like syndrome.
Isoniazid
3
9
Vancomycin
(Vancocin)
The drug of choice
and last resort where
other antibiotics are
not effective.
Amino glycosides:
ototoxicity and
nephrotoxicity
4
0
Metronidazole
(Flagyl)
GIT(NAUSEA,VOMITING,ABDO
MINAL CRAMP)
METALIC TESTE,ORAL
YEAST INFECTION
(MONILIASIS)
WITH ALCOHOL
~FROM DISULFIRAM
LIKE EFFECT
Rifabutin &
rifapentine. (Newer)
Rifampin:
To monitor: Liver function tests.
Isoniazid:
Monitor: CBC, liver function.
Caution: Age, diabetes, HIV,
uremia, alcoholism, malnutrition,
pregnancy, seizure disorder
,NEUROTOXICOLOGIC
PROBLEM
(DIZZINESS,VERTIGO AND
NUMBNESS)
4
1
Polyene Antibiotics
Imidazole
(Miconazole,Ketocona
zole
Clotrimazole
,Econazole,
Mebendazole
,Oxiconazole
Thiabendazole
,Tiaconazole)
Triazole
(Fluconazole
,Itraconazole)
Allyalamine
(Terbinafine; Lamisil)
ALLERGY,GIT DISTURBANCE ,
GYNECOMASTIA AND
IMPOTANCE.
HEPATIC DYSFUNCTION AND
LIVER MICROSOMAL ENZYME
INHIBITOR
OTHER AZOLES~ LESS SIDE
EFFECT
FLUCONAZOLE~ NO
ENDOCRINE SIDE EFFECT
4
2
Quniolones and
Fluoroquinolones
Antibiotics
Ciprofloxacin (Cipro)
Levofloxacin
(Levaquin)
Norfloxacin (Noroxin)
Ofloxacin (Floxin)
Moxifloxacin (Avelox)
Gatifloxacin (tequin)
GIT(NAUSEA,VOMITING,DIARR
HEA)
CNS(DIZZINESS,HEADACHE,SE
IZURE)
PHOTOTOXICITY
GATIFLOXACIN~ DIABETES
GREPAFLOXACIN~
PROLONGED QTINTERVAL
TROVAFLOXACIN~ FETAL
LIVER DAMAG
THEOPHYLLINE~
INCREASE
CIPROFLOXACINE
CONCENTRATION
DECREASE CATIONS
( AL,Mg,Ca,Zn,Fe)
ABSORPTION
4
3
Macrolides
Antibiotics
GIT:(NAUSEA,VOMITING
,DIARRHIEA)
MICROSOMAL
ENZYME INHIBITER
(erythromycin
,clarithromycin
azithromycin
roxithromycin)
The macrolides are a
group of drugs
(typically antibiotics)
whose activity stems
from the presence of
a macrolide ring, a
large lactone ring
to which one or
more
deoxy sugars,
usually cladinose and
desosamine, are
attached. The
lactone ring can be
either 14, 15 or 16membered.
Macrolides belong to
the polyketide class
of
natural products.
LIVER: CHOLESTATIC
JAUNDICE
OTOTOXCIT
~INCREASE
WARFARINE TOXICITY
4
4
Aminoglycosides
Amikacin,
gentamicin,
kanamycin,
neomycin,
streptomycin, and
tobramycin.
OTOTOXICITY
,NEPHROTOXICITY ,SKELETAL
MUSCLE RELAXANT ,ALLERGIC
REACTION
CEPHALOSPORINS,
POLYMYXINS AND
FUROSAMDE.
4
5
Finasteride
(Propecia):
Antiandrogen
5 alpha reductase
inhibitor
4
6
4
7
Flutamide
Bicalutamide
(Casodex)
Nilutamide
(Anandron)
Tetracyclines
Doxycylcine
Demeclomycin
Minocycline
swelling or tenderness in
breasts, dizziness)
eta Lactam
Antibiotics
Penicillins
Cephalosporins
First generation
cephalosporins
cephalexin
,cephalothin
cephazolin
Second generation
cephalosporins
cefaclor ,cefuroxime
cefamandole
Second generation
cephamycins
Moderate
spectrum with
anti-anaerobic
activity.
cefotetan , cefoxitin
Third generation
cephalosporins
Broad spectrum.
ceftriaxone ,
cefotaxime
Broad spectrum
with anti-
GIT(ANOREXIA,EPIGASTRIC
PAIN, ABDOMINAL DISTENTION
,PERIANAL
IRRITATION),CLACIFIED
TISSUE,FETAL HEPATOTOXICITY
PHOTOSENSITIVTY,
AZOTEMIA,FAN-CNI
SYNDROME(TETRACYCLINE~E
PITETRACYCLINE~ LEADE TO
NAUSEA ,VOMITING,POLYURIA,
POLYDIPSIA,PROTEINEURIA
,ACIDOSIS AND GLYCOSURIA
Penicillins: Hypersensitivity
reactions (urticarial, vesicular,
bullous, scarlatiniform,
maculopapular. Thrombopenic
purpura, fever, eosinophilia,
angioedema, serum sickness).
Anaphylaxis: (severe
hypotension,
bronchoconstriction, nausea,
vomiting, abdominal pain, and
extreme weakness).GI
distress, bone marrow
suppression, superinfection.
Cephalosporins:
Hypersensitivity (See for
penicillins), NVD,
superinfection, nephrotoxicity,
Clostridium difficileinduced
colitis.
Cefoperazone, cefmetazole,
cefotetan: bleeding diatheses.
Penicillins:
Probenecid.
Antagonism:
Erythromycins,
tetracyclines, or
chloramphenicol.
Parenteral products
contain either
potassium, sodium.
Cephalosporins:
Cross-sensitivity with
penicillin.Probenecid
(except ceftazidime).
Alcohol consumption:
cefmetazole,
cefotetan,
cefoperazone.
Antacids Cefaclor
extended-release
tablets, cefdinir,
cefpodoxime.
H2-antagonists:
cefpodoxime &
cefuroxime.
Iron supplements and
iron-fortified foods:
cefdinir
Penicillins:
A positive history for reactions
Renal impairment.
Procaine hypersensitivity is a
contraindication to the use of
procaine penicillin G.
Cephalosporins:
Ceftriaxone: Newborns receiving
concurrent administration of
calcium containing solutions.
IV calcium-containing solutions.
Carbapenems:
Cross-sensitivity reactions those
are allergic to penicillin or
cephalosporins
Pseudomonas
activity.
ceftazidime
Fourth generation
cephalosporins
cefepime
Carbapenems
4
8
Analgesics:
Narcotics
Endogenous
opioids
Opioid-peptides that
are produced in the
body:endorphins
dynorphins
enkephalins
Opium alkaloids
Phenanthrenes
naturally occurring in
opium:morphine
,codeine
thebaine
Semisynthetic
derivatives
diamorphine
(heroin) , oxycodone
hydrocodone
,dihydrocodeine
hydromorphone
,oxymorphone
Synthetic opioids
Phenylheptylamine
s
methadone
levomethadyl
acetate
hydrochloride
Phenylpiperidines
pethidine
(meperidine)
fentanyl , alfentanil
sufentanil
facilitated by transpeptidases
known as penicillin binding proteins
(PBPs). Inhibition of PBPs may also
lead to the activation of autolytic
enzymes in the bacterial cell wall.
-lactam antibiotics are indicated
for the prophylaxis and treatment
of bacterial infections caused by
susceptible organisms.
An opioid is any agent that binds to
opioid receptors found principally in
the central nervous system and
gastrointestinal tract. There are
four broad classes of opioids:
endogenous opioid peptides,
produced in the body; opium
alkaloids, such as morphine
(the prototypical opioid) and
codeine; semi-synthetic opioids
such as heroin and oxycodone; and
fully synthetic opioids such as
pethidine and methadone that have
structures unrelated to the opium
alkaloids.
There are at least three major
classes of opioid receptors: ,
and
. These are all G-protein
coupled receptors acting on
GABAergic neurotransmission.
The receptor (the represents
morphine) is perhaps the most
important being responsible for
most of the analgesic and other
major pharmacological effects
as well as many of the adverse
effects of opioids.
Opioid overdose can be rapidly
reversed with any of several opioid
antagonists such as naloxone.
These competitive antagonists are
drugs that bind to the -opioid
receptors with higher affinity than
agonists but do not activate them.
Carbapenems: NVD,
pseudomembranous colitis,
seizures, dizziness,
hypotension.
Cephalosporins: may
cause false-positive
glycosuria results.
4
9
Diphenylpropylami
ne derivatives
propoxyphene
dextropropoxyphene
Benzomorphan
derivatives
pentazocine ,
phenazocine
Oripavine
derivatives
buprenorphine
Morphinan
derivatives
butorphanol,
nalbufine
tramadol, loperamide
diphenoxylate
Opioid antagonists
naloxone , naltrexone
Gout
Colchicine
Allopurinol
Colchicine:
NVD, abdominal pain,
myopathy, neutropenia,
aplastic anemia, alopecia.
Allopurinol: Hypersensitivity
runs in skin. Acute attacks of
gout. Colchicine and NSAIDS:
NV.
Pregnancy.
Caution: hepatic, renal, or
cardiovascular disease.
Allopurinol
6-mercaptopurine,
azathioprine.