GENERAL CLASSIFICATION: Histamine 2 (H2) Receptor Antagonists

Brand name(s): Tagamet

Drug Structure: C10H16N6S

MECHANISM OF ACTION

H2 receptor antagonists decrease gastric acid secretion by reversibly binding to histamine H2 receptors located on gastric parietal cells, thereby inhibiting the binding and action of
the endogenous ligand histamine, as well as acting on the H2 receptors of the CNS to prevent or mediate the postsynaptic actions of histamine (e.g. itching, secretions from nasal
mucosa, formation of edema and stimulation of sensory nerve endings, etc.).

DRAWING/ILLUSTRATION
 PHARMACOKINETICS

INDICATIONS
ABSORPTION DISTRIBUTION METABOLISM EXCRETION (WITH CONTRAINDICA DRUG ADVERSE
DRUGS DOSAGE) TIONS INTERACTIONS EFFECTS

GENERIC PO: rapidly Only a small t1/2 = 1 to 3.5 Excreted through -Promotes - Use with Inhibits CYPs Diarrhea,
NAME: absorbed fraction is protein hours (Adults) the kidneys by healing of gastric caution in and increases headache,
Cimetidine bound. filtration and and duodenal pregnant women the levels of drowsiness,
Tmax: 1 to 3 Children: renal tubular ulcers. - Several reports drugs that are fatigue, muscular
 hours reduced by about secretion. -Prevents the have associated substrates for pain,
30% occurrence of H 2 receptor these enzymes. constipation
Enhanced by stress ulcers antagonists with
food or various blood
decreased by disorders,
antacids including
thrombocytopeni
a

FAMILY: DURATION OF IV Route -

ACTION: 4 to 5 Intermittent
hrs after IV bolus: 300 mg
dosing. every 6–8 h
-Continuous
infusion: 37.5–
100 mg/h
Note: use in
critically ill
patients

Oral Route:
-Adult Dosage:
400 mg 4 times
daily or 800 mg
twice daily for 12
weeks
-Pediatric: 20–40
mg/kg/d divided
every 6 h for 8–
12 weeks
GENERAL CLASSIFICATION: Histamine 2 (H2) Receptor Antagonists

Brand name(s): Zantac (Ranitidine)

Drug Structure: C13H22N4O3S

MECHANISM OF ACTION

H2 receptor antagonists decrease gastric acid secretion by reversibly binding to histamine H2 receptors located on gastric parietal cells, thereby inhibiting the binding and action of
the endogenous ligand histamine, as well as acting on the H2 receptors of the CNS to prevent or mediate the postsynaptic actions of histamine (e.g. itching, secretions from nasal
mucosa, formation of edema and stimulation of sensory nerve endings, etc.).

DRAWING/ILLUSTRATION

PHARMACOKINETICS

INDICATIONS
ABSORPTION DISTRIBUTION METABOLISM EXCRETION (WITH CONTRAINDICA DRUG ADVERSE
DRUGS DOSAGE) TIONS INTERACTIONS EFFECTS

GENERIC PO: rapidly Only a small t1/2 = 1 to 3.5 Excreted through -Promotes - Use with Interacts with Diarrhea,
NAME: absorbed fraction is protein hours (Adults) the kidneys by healing of gastric caution in hepatic CYPs; headache,
Ranitidine bound. filtration and and duodenal pregnant women affinity only 10% drowsiness,
 Tmax: 1 to 3 renal tubular ulcers. - Several reports of that of fatigue, muscular
hours secretion. -Prevents the have associated cimetidine. pain,
occurrence of H 2 receptor constipation
Enhanced by stress ulcers antagonists with
food or various blood
decreased by disorders,
antacids including
thrombocytopeni
a

CLASSIFICATIO ONSET: IV Route Interacts with Confusion,

N: -Intermittent alcohol to cause delirium,
bolus: 50 mg slight increase in hallucinations,
every 6–8 h blood alcohol slurred speech,
-Continuous concentration. headaches (less
infusion: 6.25– common; occur
12.5 mg/h primarily with IV
administration or
in elderly)

FAMILY: DURATION OF Oral Route:

ACTION: 6 to 8 -Adult Dosage:
hrs after IV 150 mg twice
dosing. daily
-Pediatric: 5–10
mg/kg/d divided,
every 8–12 h
GENERAL CLASSIFICATION: Histamine 2 (H2) Receptor Antagonists

Brand name(s): Pepcid (Famotidine)

Drug Structure: C8H15N7O2S3

MECHANISM OF ACTION

H2 receptor antagonists decrease gastric acid secretion by reversibly binding to histamine H2 receptors located on gastric parietal cells, thereby inhibiting the binding and action of
the endogenous ligand histamine, as well as acting on the H2 receptors of the CNS to prevent or mediate the postsynaptic actions of histamine (e.g. itching, secretions from nasal
mucosa, formation of edema and stimulation of sensory nerve endings, etc.).

DRAWING/ILLUSTRATION

PHARMACOKINETICS

INDICATIONS
ABSORPTION DISTRIBUTION METABOLISM EXCRETION (WITH CONTRAINDICA DRUG ADVERSE
DRUGS DOSAGE) TIONS INTERACTIONS EFFECTS

GENERIC PO: rapidly Only a small t1/2 = 1 to 3.5 Excreted through -Promotes - Use with Interacts with Diarrhea,
NAME: absorbed fraction is protein hours (Adults) the kidneys by healing of gastric caution in hepatic CYPs; headache,
Famotidine bound. filtration and and duodenal pregnant women safer to use drowsiness,
 Tmax: 1 to 3 renal tubular ulcers. - Several reports compared to fatigue, muscular
hours secretion. -Prevents the have associated ranitidine. pain,
occurrence of H 2 receptor constipation
stress ulcers antagonists with
Enhanced by various blood
food or disorders,
decreased by including
antacids thrombocytopeni
a

CLASSIFICATIO ONSET: IV Route Interacts with Confusion,

N: -Intermittent alcohol to cause delirium,
bolus: 20 mg slight increase in hallucinations,
every 12 h blood alcohol slurred speech,
-Continuous concentration. headaches (less
infusion: 1.7–2.1 common; occur
mg/h primarily with IV
administration or
in elderly)

FAMILY: DURATION OF Oral Route:

ACTION: 10 to -Adult Dosage:
12 hrs after IV 20 mg twice daily
dosing. for up to 12
weeks
-Pediatric: 0.5
mg/kg/d at
bedtime or
divided every 12
h (infants < 3
months)
GENERAL CLASSIFICATION: Histamine 2 (H2) Receptor Antagonists

Brand name(s): Axid, Tazac (Nizatidine)

Drug Structure: C12H21N5O2S2

MECHANISM OF ACTION

H2 receptor antagonists decrease gastric acid secretion by reversibly binding to histamine H2 receptors located on gastric parietal cells, thereby inhibiting the binding and action of
the endogenous ligand histamine, as well as acting on the H2 receptors of the CNS to prevent or mediate the postsynaptic actions of histamine (e.g. itching, secretions from nasal
mucosa, formation of edema and stimulation of sensory nerve endings, etc.).

DRAWING/ILLUSTRATION

PHARMACOKINETICS INDICATIONS CONTRAINDICA DRUG ADVERSE

DRUGS (WITH TIONS INTERACTIONS EFFECTS
 ABSORPTION DISTRIBUTION METABOLISM EXCRETION DOSAGE)

GENERIC PO: rapidly Only a small t1/2 = 1 to 3.5 Excreted through -Promotes - Use with Interacts with Diarrhea,
NAME: absorbed fraction is protein hours (Adults) the kidneys by healing of gastric caution in hepatic CYPs; headache,
Nizatidine bound. filtration and and duodenal pregnant women safer to use drowsiness,
Tmax: 1 to 3 renal tubular ulcers. - Several reports compared to fatigue, muscular
hours secretion. -Prevents the have associated ranitidine. pain,
occurrence of H 2 receptor constipation
Enhanced by stress ulcers antagonists with
food or various blood
decreased by disorders,
antacids including
thrombocytopeni
a

CLASSIFICATIO ONSET: Oral Route Interacts with Confusion,

N: -Adult Dosage: alcohol to cause delirium,
150 mg twice slight increase in hallucinations,
daily blood alcohol slurred speech,
-Pediatric: concentration. headaches (less
<12 years: 10 common; occur
mg/kg/dc divided primarily with IV
every 12 h >12 administration or
years: 150 mg in elderly)
twice daily

FAMILY: DURATION OF
ACTION:

GENERAL CLASSIFICATION: Local anesthetics (Amides)

Brand name(s): Lidamantle, Xylocaine (Lidocaine)

Drug Structure: C14H22N2O

MECHANISM OF ACTION

Local anesthetics act at the cell membrane to prevent the generation and
the conduction of nerve impulses. Local anesthetics block conduction by decreasing or preventing the
large transient increase in the permeability of excitable membranes to
Na+ that normally is produced by a slight depolarization of the membrane.

DRAWING/ILLUSTRATION
 PHARMACOKINETICS

INDICATIONS
ABSORPTION DISTRIBUTION METABOLISM EXCRETION (WITH CONTRAINDICA DRUG ADVERSE
DRUGS DOSAGE) TIONS INTERACTIONS EFFECTS
GENERIC Absorbed rapidly Amide-linked Terminal Dealkylated in -Lidocaine is Hypersensitivity Interacts with Drowsiness,
NAME: Lidocaine after parenteral local anesthetics elimination t1/2= 2 liver by CYP to used as a local to amide type epinephrine to tinnitus,
administration bind extensively hrs monoethylglycine anesthesia but of local decrease its rate dysgeusia,
and GI and (55% - 95%) to and xylidide. can be also used anaesthetics of absorption; dizziness,
respiratory tracts plasma proteins 75% of xylidide is in treatment for decreases twitching
particularly excreted in urine. ventricular probability of
Tmax: 2 to 5 alpha1 -acid arrythmias. toxicity and
mins (Topical glycoprotein. -Used for prolongs duration
Anesthesia) attenuation of of action.
increased
Epinephrine intracranial
decreases rate of pressure during
absorption and intubation or
increases suctioning.
duration of action -Treatment for
refractory
seizures and
status epilepticus

CLASSIFICATIO ONSET: Topical Seizures, coma,

N: Anesthesia respiratory
- 2%–10% depression,
solution: Maximal arrest (as dose
healthy adult increases)
dose, ~4 mg/kg

FAMILY: DURATION OF Infiltration

ACTION: Anesthesia
30 to 45 mins -0.5%–1.0%
(Topical solution: Maximal
Anesthesia) healthy adult
dose, ~4 mg/kg
Note: Addition of
epinephrine (5
μg/mL) increases
duration of action
and maximal
safe lidocaine
dose

Nerve Block
Anesthesia:
•Use with
epinephrine-
containing test
dose
•Risk of
intravenous
injection
•Safe doses
depend on
vascularity of
tissue, generally:
-Lidocaine: 1%–
1.5%, maximal
healthy adult
dose, ~4 mg/kg
-Mepivacaine:
1%–2%, maximal
healthy adult
dose, ~7 mg/kg
(maximum 400
mg)

Epidural
Anesthesia
• Use with
epinephrine-
containing test
dose
• Risk of
intravenous
injection
• Spread of block
dependent on
dose and volume
injected
• Epidural
catheter allows
repeated dosing
• Consider
coagulation
status of patient:
-2% solution
Maximal healthy
adult dose, ~4
mg/kg

Spinal
Anesthesia
• Dose and
baricity of
anesthetic
strongly
influence spread
• Addition of
opioids can
prolong
analgesia
• Consider
coagulation
status of patient:
-~25–50 mg for
perineal and
lower extremity
surgery
SP: Association
of spinal
lidocaine with
transient
neurological
symptoms