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DRUG HANDBOOK

PHARAMACOLOGY IN
NURSING

BY: BERMIO, RICA MAE A.


CI: EMELYN MANGAOANG, RN
CARDIOVASCULAR
SYSTEM
Generic name: CAPTOPRIL

Indications: Management of hypertension and heart failure.


Reduction of risk of death, heart failure-related hospitalizations, and
development of over heart failure following myocardial infarction.
Treatment of diabetic nephropathy in patients with Type 1 diabetes
mellitus and retinopathy. Treatment for postpartum patient with
hypertension.

Actions: Angiotensin- converting enzyme (ACE) inhibitors block


the conversion of angiotensin II. ACE inhibitors also prevent the
degradation of bradykinin and other vasodilatory prostaglandins.
ACE inhibitors also increases plasma renin levels and decreases
aldosterone levels.

Pharmacokinetics:

Route Onset Peak Duration

Oral 15-60 min 60-90 min 6-12hrs

Half time: 2hrs

Adverse effect:

Gastrointestinal (GI) tract: nausea, diarrhea

CNS: headache, dizziness, fatigue, malaise, drowsiness, weakness

Genitourinary: renal failure, proteinuria

CV: angina pectoris, tachycardia, hypotension

Hematologic: leucopenia, thrombocytopenia

Respiratory: cough, asthma, dyspnea

Skin: rash, angioedema

Other: altered taste, fever


Generic name: LOSARTAN

Indications: Losartan is used to treat high blood pressure


(hypertension). It is also used to lower the risk of strokes in patients
with high blood pressure.

Actions: It works by relaxing blood vessels so that blood can flow


more easily. The main action is to block pressure raising effect of
the renin- angiotensin- aldosterone system (RAAS).

Pharmacokinetics:

Route Onset Peak Duration

Oral 6hrs 1-2hrs 24hrs

Half time: 1.5- 2 hours

Adverse effect:

Gastrointestinal (GI) tract: nausea, diarrhea, abdominal pain, dry


mouth, tooth pain

CNS: headache, dizziness, syncope, weakness

CV: edema, chest pain

Respiratory: cough, symptoms of upper respiratory tract infections


(URTI)

EENT: rash, alopecia, dry skin, nasal congestion, sinusitis,


pharyngitis, sinus disorder
Generic name: AMLODIPINE

Indications: Angina pectoris due to coronary artery spasm, Chronic


stable angina, alone or in combination with other agents, Essential
hypertension, alone or in combination with other hypertensive.

Actions: Inhibits the movement of calcium ions across the


membranes of cardiac and arterial muscle cells; inhibits
transmembrane calcium flow, which results in the depression of
impulse formation in specialized cardiac pacemaker cells, slowing
of the velocity of conduction of the cardiac impulse, depression of
myocardial contractility, and dilation of coronary arteries, and
arterioles and peripheral arterioles; these effects lead to decreased
cardiac work, decreased cardiac oxygen consumption, and in
patients with vasospastic angina, increased delivery of oxygen to
cardiac cells.

Pharmacokinetics:

Route Onset Peak Duration

Oral 6-12hrs 6-12hrs 24hrs

Half time: 30-50 hours

Adverse effect:

Gastrointestinal (GI) tract: nausea, abdominal discomfort

CNS: headache, dizziness, lightheadedness, asthenia, fatigue,


lethargy

CV: peripheral edema, arrhythmias

Dermatologic: flushing, rash


Generic name: HYDRALAZINE

Indications: Essential hypertension. To manage hypertensive


emergencies related to pregnancy (pre-eclampsia or eclampsia). To
manage severe heart failure.

Actions: Acts directly on vascular smooth muscle to cause


vasodilation, primarily arteriolar, decreasing peripheral resistance;
maintains or increases renal and cerebral blood flow.

Pharmacokinetics:

Route Onset Peak Duration

IV Rapid 10-20mins 2-4hrs

IM Rapid 10-20mins 2-4hrs

Oral Rapid 1-2hrs 6-12hrs

Half time: 2-8 hours

Adverse effect:

Gastrointestinal (GI) tract: anorexia, nausea, vomiting, diarrhea

CNS: headache, dizziness, peripheral neuritis

CV: palpitations, tachycardia, angina pectoris

GU: difficult maturation, impotence

Hematologic: blood dyscrasias

Hypersensitivity: rash, urticaria, pruritus

Other: nasal congestion, flushing, edema, muscle cramps


Generic name: LISINOPRIL

Indications: Zestril is indicated for the treatment of hypertension in


adult patients and pediatric patients 6 years of age and older to
lower blood pressure.

Lowering blood pressure lowers the risk of fatal and non-fatal


cardiovascular events, primarily stroke and myocardial infractions.
These benefits have been seen in controlled trials of
antihypertensive drugs from a wide variety of pharmacologic
classes.

Actions: Blocks the conversion of angiotensin II, increases the


plasma renin levels and reduces aldosterone levels. Net result is
systemic vasolidation, lowers the blood pressure.

Pharmacokinetics:

Route Onset Peak Duration

Oral 1-2hrs 6hrs 6weeks

Half time: 12 hours

Adverse effect:

Gastrointestinal (GI) tract: abdominal pain, nausea, dry mouth,


diarrhea, tooth pain

CNS: headache, dizziness, syncope, weakness

Respiratory: symptoms of upper respiratory tract infections

(URTI), cough

EENT: rash, alopecia, dry skin


IMMUNE
SYSTEM
Generic name: ACETAMINOPHEN

Indications: Analgesic-antipyretic in patients with aspirin allergy,


hemostatic disturbances, bleeding diatheses, upper GI disease, gouty
arthritis. Arthritis and rheumatic disorders involving musculoskeletal pain
(but lacks clinically significant anti-rheumatic and anti-inflammatory
effects). Common cold, flu, other viral and bacterial infections with pain
and fever. Unlabeled use: Prophylactic for children receiving DPT
vaccination to reduce incidence of fever and pain.

Actions: Antipyretic: reduces fever by acting directly on the hypothalamic


heat-regulating center to cause vasodilation and sweating, which helps
dissipate heat. Analgesic: site and mechanism of action unclear.

Pharmacokinetics:

Route Onset Peak Duration

Oral 30-45minis 0.5-2hrs 4-6hrs

Half time: 2hrs

Adverse effect:

Gastrointestinal (GI) tract: Hepatic toxicity and failure, jaundice

CNS: agitation, anxiety, dizziness, insomnia, headache, pyrexia, fatigue

CV: Chest pain, dyspnea, myocardial damage, hypotension, peripheral


edema, periorbital edema

GU: Acute kidney failure, renal tubular necrosis

Hematologic: Methemoglobinemia-cyanosis; hemolytic anemia- hematuria,


anuria; neutropenia, leukopenia, pancytopenia, thrombocytopenia,
hypoglycemia

Hypersensitivity: rash, fever


Generic name: ASPIRIN

Indications: Treatment of mild to moderate pain, fever, numerous


inflammatory conditions (e.g., rheumatoid arthritis and osteoarthritis).
Mesalamine and balsalazide are indicated for ulcerative colitis and other
inflammatory bowel conditions in adults. Sodium thiosalicylate is used in
treatment of arthritis and muscular pain.

Actions: It inhibits synthesis of prostaglandin, an inflammatory reaction


mediator. Antipyretic effect is through blocking of prostaglandin mediator
of pyrogens (chemicals released by active white blood cells that cause
increase in body temperature) at the thermoregulatory center of the
hypothalamus. Aspirin at low levels can affect reduce platelet aggregation
by inhibiting synthesis of thromboxane A2, a potent vasoconstrictor that
normally increases platelet aggregation and blood clot formation. On the
other hand, at higher levels, it inhibits the synthesis of prostacyclin, a
vasodilator that inhibits platelet aggregation.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 5-30mins 0.25-2hrs 3-6hrs
RECTAL 1-2hrs 4-5hrs 6-8hrs

Half time: 15mins-12hrs

Adverse effect:

Gastrointestinal (GI) tract: nausea, dyspepsia, heartburn, epigastric


discomfort

Hematological: blood loss, bleeding abnormalities

Salicylism can occur with high levels of aspirin characterized by dizziness,


ringing in the ears, difficulty hearing, nausea, vomiting, diarrhea, mental
confusion, and lassitude.

Acute salicylate toxicity occurs at doses of 20-25 g in adults or 4 g in


children. Signs include hyperpnea, tachypnea, hemorrhage, excitement,
confusion, pulmonary edema, convulsions, tetany, metabolic acidosis, fever,
coma, and cardiovascular (CV), renal, and respiratory collapse.
Generic name: IBUPROFEN

Indications: To reduce fever and to relieve mild to moderate pain and


inflammation associated with dysmenorrhea, headache including migraine,
post- operative pain, dental pain and musculoskeletal and joint disorders
such as ankylosing spondylitis, osteoarthritis and rheumatoid arthritis
including juvenile idiopathic arthritis.

Actions: Prototype of the propionic acid NSAIDs (cox-1) inhibitor with


nonsteroidal anti- inflammatory activity and significant antipyretic and
analgesic properties. Blocks prostaglandin synthesis. Ibuprofen activity also
includes modulation of T-cell function, inhibition of inflammatory cell
chemotaxis, decreased release of superoxide radicals, or increased
scavenging of these compounds at inflammatory sites.

Pharmacokinetics:
Route Onset Peak Duration
Oral 1 h antipyretic 1-2hrs 6-8hrs

Half time: 1.9 to 2.2hrs

Adverse effect:
Gastrointestinal (GI) tract: abdominal pain, diarrhea- nausea, vomiting,
GI bleeding- ulceration

CNS: headache, dizziness, light-headedness, anxiety, emotional lability,


fatigue, malaise, drowsiness, anxiety, confusion

Genitourinary: acute renal failure, polyuria, azotemia, cystitis, hematuria,


nephrotoxicity, decreased creatinine clearance
Generic name: NAPROXEN

Indications: Naproxen is indicated for the management of rheumatoid


arthritis, osteoarthritis, ankylosing spondylitis, polyarticular juvenile
idiopathic arthritis, tendinitis, bursitis, acute gout, primary dysmenorrhea,
and for the relief of mild to moderate pain. Further, it is first-line therapy for
osteoarthritis, acute gouty arthritis, dysmenorrhea, and musculoskeletal
inflammation and pain.

Actions: As with other non-selective NSAIDs, naproxen exerts it's clinical


effects by blocking COX-1 and COX-2 enzymes leading to decreased
prostaglandin synthesis.3 Although both enzymes contribute to
prostaglandin production, they have unique functional differences.3 The
COX-1 enzymes is constitutively active and can be found in normal tissues
such as the stomach lining, while the COX-2 enzyme is inducible and
produces prostaglandins that mediate pain, fever and inflammation. The
COX-2 enzyme mediates the desired antipyretic, analgesic and anti-
inflammatory properties offered by Naproxen, while undesired adverse
effects such as gastrointestinal upset and renal toxicities are linked to the
COX-1 enzyme.

Pharmacokinetics:
Route Onset Peak Duration
Oral 1hr 5hrs 8-12hrs

Half time: 12-17 hours

Adverse effect:

Gastrointestinal (GI) tract: nausea, dyspepsia, GI pain

CNS: headache, dizziness, insomnia, somnolence

Dermatologic: rash, pruritus, stomatitis

Respiratory: dyspnea, hemoptysis, bronchospasm

Other: peripheral edema


Generic name: METHOTREXATE

Indications: To treat severe psoriasis unresponsive to other therapy. To


treat severe rheumatoid arthritis unresponsive to other therapy. To treat
active polyarticular juvenile idiopathic arthritis.

Actions: May exert immunosuppressive effects by inhibiting replication


and function of T and possibly B lymphocytes. Methotrexate also slows
rapidly growing cells, such as epithelial skin cells in psoriasis.

Pharmacokinetics:
Route Onset Peak Duration
Oral 3-6wks Unknown Unknown
IV 3-6wks Unknown Unknown
IM 3-6wks Unknown Unknown

Half time: 2.5 to 5 mg every 12hrs for 3 doses/week, increased as ordered


by 2.5 mg/week.

Adverse effect:
 aphasia, cerebral thrombosis, chills, dizziness, drowsiness,
fatigue, fever, headache, hemiparesis, leukoencephalopathy,
malaise, paresis, seizures
RENAL
SYSTEM
Generic name: HYDROCHLOROTIAZIDE

Indications: Hydrochlorothiazide is indicated alone or in combination for the


management of edema associated with congestive heart failure, hepatic cirrhosis,
nephrotic syndrome, acute
glomerulonephritis, chronic renal failure, and corticosteroid and estrogen therapy.
Hydrochlorothiazide is also indicated alone or in combination for the management of
hypertension.

Actions: Interference with the renal tubular mechanism of electrolyte reabsorption.


Thiazides increase excretion of sodium and chloride in approximately equivalent
amounts. Natriuresis causes a secondary loss of potassium and bicarbonate.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 2hrs 3-6hrs 6-12hrs

Half time: 8-15 hours

Adverse effect:
Gastrointestinal (GI) tract: anorexia, nausea, pancreatitis, epigastric distress,
vomiting, abdominal pain, diarrhea, constipation

CNS: dizziness, vertigo, headache, paresthesia, weakness, restlessness


CV: orthostatic hypotension, vasculitis.

GU: polyuria, frequent urination, renal failure, interstitial nephritis

Hematologic: aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia,


hemolytic anemia

Hepatic: jaundice

Metabolism: hypokalemia; asymptomatic hyperuricemia; hyperglycemia and


impaired glucose tolerance; fluid and electrolyte imbalances, including dilutional
hyponatremia hypochloremia, metabolic alkalosis, hypercalcemia

Musculoskeletal: muscle cramps

Respiratory: respiratory distress, pneumonitis.

Skin: dermatitis, photosensitivity, rash, purpura, alopecia


Generic name: FUROSEMIDE

Indications: Edema due to heart failure, hepatic impairment, or renal disease.


Hypertension.

Actions: Inhibits the reabsorption of sodium and chloride from the loop of Henle and
distal renal tubule. Increases renal excretion of water, sodium, chloride, magnesium,
potassium, and calcium. Effectiveness persists in impaired renal function.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 30-60mins 1-2hrs 6-8hrs
IM 10-30mins unknown 4-8hrs
IV 5mins 30mins 2hrs

Half time: 30-60mins (increase in renal impairment)


Adverse effect:
CV: hypotension

Derm: erythema multiforme, stevens-johnson syndrome, toxic epidermal necrolysis,


photosensitivity, pruritus, rash, urticaria

EENT: hearing loss, tinnitus

Endo: hypercholesterolemia, hyperglycemia, hypertriglyceridemia, hyperuricemia

F and E: dehydration, hypocalcemia, hypochloremia, hypokalemia,


hypomagnesemia, hyponatremia, hypovolemia, metabolic alkalosis
GI: anorexia, constipation, diarrhea, dry mouth, dyspepsia, ↑ liver enzymes, nausea,
pancreatitis, vomiting

GU: ↑ BUN, excessive urination, nephrocalcinosis

Hemat: aplastic anemia, agranulocytosis, hemolytic anemia, leukopenia,


thrombocytopenia

MS: muscle cramps

Neuro: paresthesia, blurred vision, dizziness, headache, vertigo

Misc: fever
Generic name: ACETAZOLAMIDE

Indications: Lowering of intraocular pressure in the treatment of glaucoma.


Management of acute altitude sickness. Edema due to HF. Adjunct to the treatment of
refractory seizures.

Actions: Inhibition of carbonic anhydrase in the eye results in decreased secretion of


aqueous humor. Inhibition of renal carbonic anhydrase, resulting in self-limiting
urinary excretion of sodium, potassium, bicarbonate, and water. CNS inhibition of
carbonican- hydrase and resultant diuresis may decrease abnormal neuronal firing.
Alkaline diuresis prevents precipitation of uric acid or cystine in the urinary tract.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 1-5hrs 2-4hrs 8-12hrs
PO-ER 2hrs 8-18hrs 18-24hrs
IV 2mins 15mins 4-5hrs

Half time: 2.4-5.8 HOURS

Adverse effect:

CNS: depression, fatigue, weakness, drowsiness

Derm: stevens-johnson syndrome, rashes

EENT: transient nearsightedness

F and E: hyperchloremic, acidosis, hypokalemia, growth retardation (in children


receiving chronic theraphy)

GI: anorexia, metallic taste, nausea, vomiting, melena

GU: crytalluria, renal calculi

Hemat: aplastic anemia, hemolytic anemia, leukopenia

Metab: weight loss, hyperuricemia

Neuro: paresthesia

Misc: allergic reactions including anaphylaxis


Generic name: OXYBUTYNIN

Indications: Relief of symptoms of bladder instability associated with


voiding in patients with uninhibited neurogenic and reflex neurogenic
bladder. ER tablets: treatment of signs and symptoms of overactive bladder
(incontinence, urgency, frequency).

Actions: Acts directly to relax smooth muscle and inhibits the effects of
acetylcholine at muscarinic receptors; reported to be less potent an
anticholinergic than atropine but more potent as antispasmodic and devoid
of antinicotinic activity at skeletal neuromuscular junctions or autonomic
ganglia.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 30-60mins 3-6hrs 6-10hrs
Transdermal 24-48hrs varies 96hrs

Half time: 2-3 HOURS

Adverse effect:
 stomach pain (especially after meals), feeling sick or being sick, a
persistent urge to poo, not being able to poo or you have runny
poos – these are all signs of faecal impaction, where large,
hardened poo gets stuck and you cannot push it out, difficulty
fully emptying your bladder, or difficulty in starting to pee – these
are signs of urinary retention, where pee builds up in your bladder
because you're unable to pee, high temperature or chills, burning
sensation when peeing, pain in your back or side, or bloody or
cloudy pee – these can be signs of a severe urinary tract infection
(UTI), swollen ankles or legs (oedema) – where fluid builds up in
your legs.
Generic name: HYDROFLUMETHIAZIDE

Indications: Used as adjunctive therapy in edema associated


with congestive heart failure, hepatic cirrhosis, and
corticosteroid and estrogen therapy.

Actions: Inhibits water reabsorption in the nephron by


inhibiting the sodium-chloride symporter in the distal
convoluted tubule, which is responsible for 5% of total
sodium reabsorption.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 2hrs 1-4hrs up to 24hrs

Half time: Alpha-phase of about 2 hours and Beta-phase of


about 17 hours

Adverse effect:
 low blood sodium or potassium levels, an imbalance
of sodium and potassium in the blood, high blood
sugar, low blood pressure, sun sensitive skin, loss of
apetite, nausea, vomiting
RESPIRATORY
SYSTEM
Generic Name: TRUPHYLINE

Indications: Relief of symptoms or prevention of bronchial asthma.


Reversal of
broncho spasm associated with COPD.

Actions: Direct effect on the smooth muscles of the respiratory


tract, both in the
bronchi and in the blood vessels. Stimulating two prostaglandins,
resulting in smooth
muscle relaxation, which increases the vital capacity that has been
impaired by the
bronchospasm or air trapping. Also inhibit the release of
slowreacting substance of
anaphylaxis and mistamine, decreasing the bronchial swelling and
narrowing that
occurs as a result of these two chemicals.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 1-6hrs 4-6hrs 6-8hrs
IV Immediate 30mins 4-8hrs

Half time: 3-15 hours (nonsmoker), 4-5 hours (smoker)

Adverse effect:

CNS: dizziness, restlessness, irritability

Cardiovascular: palpitations, life-threatening arrhythmias

GU: proteinuria

Respiratory: respiratory arrest

Others: loss of apetite, fever, flushing


Generic name: ISPROTERENOL

Indications: Long-acting treatment and prophylaxis of bronchospasm and


prevention
of exercise-induced bronchospasm in patients 2 years and older. Long-term
maintenance treatment of bronchoconstriction in COPD. Treatment of acute
bronchospasm in adults and children. Treatment and prophylaxis of acute
asthma
attacks in children more than 6 years old.

Actions: drug of choice for adults and children for the treatment of acute
bronchospasm, including that caused bypnaphylaxis; it is also available for
inhalation. At therapeutic levels, the action of most sympathomimetics are
specific to
the beta-receptors found in the bronchi.

Pharmacokinetics:
Route Onset Peak Duration
SC 5-10mins 20mins 20- 30mins
IM 5-10mins 20mins 20- 30mins
IV Instant 20mins 20- 30mins
Inhalation 3-5mins 20mins 1-3hrs

Half time: unknown

Adverse effect:

CNS: dizziness, headache

GI: nausea, gastrointestinal distress

Cardiovascular: palpitations

Respiratory: cough

Misc: nervousness
Generic name: GUIFENESIN

Indication: Symptomatic relief of respiratory conditions


characterized by a dty, nonproductive cough.

Actions: Enhances the output of respiratory tract fluids by


reducing the adhesiveness
and surface tension of these fluids, allowing easier movement
of the less viscous
secretions.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 30mins Unknown 4-6hrs

Half time: unknown

Adverse effect:

CNS: dizziness, headache

GI: nausea, vomiting

Underlying cough: The most important consideration in the


use of these drugs is
discovering the cause of the underlying cough; prolonged use
of the OTC
preparations could result in the masking of important
symptoms of a serious
underlying disorder.
Generic name: CHLORPHENIRAMINE

Indications: Maintenance and treatment of bronchospasm for adults


with COPD. Long-term, once-daily maintenance and treatment of
bronchospasm associated with COPD in adults.

Actions: Used as bronchodilators because of their effect on the


vagus nerve, which
sis to block or antagonize the action of the neurotransmitter
acetylcholine at vagal-
mediated. receptor sites. By blocking the vagal effect, relaxation of
smooth muscle in
the bronchi occurs, leading to bronchodilation.

Pharmacokinetics:
Route Onset Peak Duration
INHALATION 15mins 1-2hrs 3-4hrs

Half time: unknown

Adverse effect:

CNS: dizziness, headache

GI: nausea, gastrointestinal distress

Cardiovascular: palpitations

Respiratory: cough

Misc: nervousness
Generic name: AMBROXOL

Indications: Liquefaction of secretions in high-risk respiratory


patients who have difficulty moving secretions including
postoperative patients; Clearing of secretions for diagnostic tests;
Treatment of atelectasis from thick mucus secretions.

Actions: Protect liver cells from being damaged during episodes of


acetaminophen
toxicity because it normalizes hepatic glutathione levels and binds
with a reactive
hepatotoxic metabolite of acetaminophen; Affects the mucoproteins
in the respiratory
secretions by splitting apart disulfide bonds that are responsible for
holding the
mucus material together.

Pharmacokinetics:
Route Onset Peak Duration
INHALATION 1min 5-10mins 2-
3hrs
ORAL 30-60mins 1-2hrs Unknown

Half time: 6.25 hours

Adverse effect:

CNS: dizziness, headache

GI: nausea, vomiting, anorexia

Respiratory: rhinorrhea, bronchospasm

Skin: rash
GASTROINTESTINAL
(GI) SYSTEM
Generic name: OMEPRAZOLE

Indications: Short-term treatment of active duodenal ulcer; First-line


therapy in treatment of heartburn or symptoms of gastro esophageal reflux
disease(GERD); Short-term treatment of active benign gastric ulcer; GERD,
severe erosive esophagitis, poorly responsive symptomatic GERD; Long-
term therapy: Treatment of pathologic hyper secretory conditions
(Zollinger-Ellison syndrome, multiple adenomas, systemic mastocytosis);
Eradication of H. pylori with amoxicillin or metronidazole.

Actions: Gastric acid- pump inhibitor: suppresses gastric acid secretion by a


specific inhibition of the hydrogen- potassium ATP as enzyme system at the
secretory surface of the gastric parietal cells; blocks the final step of acid
production.

Pharmacokinetics:
Route Onset Peak Duration
ORAL w/in 2hrs w/in 1hr 72-96hrs

Half time: less than 1 hour

Adverse effect:
 Diarrhea, nausea, fatigue, constipation, vomiting, flatulence, acid
regurgitation, taste perversion, arthralgia, myalgia, urticaria, dry
mouth, dizziness, headache, paraesthesia, abdominal pain, skin
rashes, weakness, back pain, upper respiratory infection, cough.
Generic name: ALUMINUM HYDROXIDE/ MAGNESIUM
HYDROXIDE

Indications: Useful in a variety of GI complaints, including: Hyperacidity,


Indigestion, GERD, Heartburn.

Actions: Neutralize gastric following dissolution in gastric contents.


Inactive pepsin if ph is raised to >4.

Pharmacokinetics:
Route Onset Peak Duration
Aluminum PO slightly delayed 30min 30min-1hr
30mins (empty
stomach); 3hrs
(after meals)
Magnesium PO slightly delayed 30 min 30min-1hr
(empty stomach);
3hrs (after meals)

Half time: Unknown

Adverse effect:

GI (most frequent): Aluminum salts: constipation


Magnesium salts: diarrhea

F and E: Magnesium salts: hypermagnesemnia


Aluminum salts: hypophosphatemia
Generic name: LANSOPRAZOLE

Indications: Short- term treatment of active duodenal ulcer; Short-term


treatment of gastro esophageal reflux disease: severe erosive esophagitis;
poorly responsive symptomatic gastroesophageal reflux disease. Treatment
of pathological hyper secretory conditions, long- term therapy. Eradication
of Helicobacter pylori infection in patients with active or recurrent duodenal
ulcers in combination with clarithromycin and amoxicillin.

Actions: Gastric pump inhibitor: Supresses gastric acid secretion by


specific inhibition of the hydrogen- potassium ATPase enzyme parietal
cells; blocks the final step of acid production.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 2-3hrs ff 1-2hr 24+hrs
a single
15mg dose;
1-2hrs ff
a single
30mg dose

Half time: 1.3- 1.7 hours

Adverse effect:
 Headache, dizziness, asthenia, vertigo, insomnia, anxiety,
paresthesias, dream abnormalities, rash, inflammation, urticarial,
pruritus, alopecia, dry skin, acne, Diarrhea, abdominal pain,
nausea, vomiting, constipation, dry mouth, URI symptoms,
cough, epistaxis, Gastric cancer in preclinical studies, back pain,
fever.
Generic name: DEXLANSOPRAZOLE

Indications: For healing all grades of erosive esophagitis (EEI),


maintaining and healing of EE and relief of heartburn, and treating
heartburn associated with symptomatic non- erosive gastroesophageal
reflux disease (GERD).

Actions: It blocks the final step of gastric acid secretion by specific


inhibition of the (H+, K+)- ATPase at the secretory surface of the parietal
cells on gastric mucosa.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 1-2hrs 4-5hrs 8wks

Half time: 1-2 hours in healthy subjects and in patients with symptomatic
GERD.

Adverse effect:
 Burning, crawling, itching, numbness, prickling, “pins and
needles” or tingling feelings, chest pain, discomfort, tightness or
heaviness, joint pain, stiffness or swelling, continuing stomach
pain.
Generic name: RABEPRAZOLE

Indications: To treat the symptoms of gastroesophageal reflux disease


(GERD), a condition in which backward flow of acid from the stomach
causes heartburn and possible injury of the esophagus.

Actions: Blocks the final step of acid gastric secretion. In gastric parietal
cells, rabeprazole is protonated, accumulates, and is transformed to an
active sulfonamide.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 5mins 1.5hrs 4wks

Half time: about 1 hour

Adverse effect:
 Bloating or swelling of the face, arms, hands, lower legs or feet,
general feeling of tiredness and weakness, hoarseness, light-
colored stools, rapid weight gain, tingling of the hands or feet,
unusual weight gain or loss, yellow eyes and skin.
CNS and PNS
SYSTEM
Generic name: DIAZEPAM

Indications: It is a fast- acting, long- lasting benzodiazepine


commonly used in the treatment of anxiety disorders, as well as
alcohol detoxification, acute recurrent seizures, severe muscle
spasm, and spasticity associated with neurologic disorders. In the
setting of acute alcohol withdrawal, diazepam is useful for
symptomatic relief of agitation, tremor, alcoholic hallucinosis, and
acute delirium tremens.

Actions: Benzodiazepines exert their effects by facilitating the


activity of GABA at various sites. Specifically, benzodiazepines
bind at an allosteric site at the interface between the alpha and
gamma subunits on GABA- A receptor chloride ion channels. The
allosteric binding of diazepam at the GABA-A receptor leads to an
increase in the frequency at which the chloride channel opens,
leading to an increased conductance of chloride ions. This shift in
charge leads to a hyperpolarization of the neuronal membrane and
reduced excitability of the neuron.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 30-60mins 1-2hrs 3hrs
IM 15-30mins 30-45mins 3hrs
IV 1-5mins 30mins 15-60mins
RECTAL rapid 1.5hr 3hrs

Half time: 20-80 hours

Adverse effect:
 Sedation, fatigue, confusion, depression, ataxia, irritability,
disinhibition, headache, tremor, dystonia, urinary retention,
incontinence, nausea, constipation, diplopia, rash,
menstrual irregularities, ALT and/or AST elevation.
Generic name: ALPRAZOLAM

Indications: Alprazolam is frequently prescribed to manage panic


and anxiety disorders.

Actions: Alprazolam belongs to a class of psycho active


medications called benzodiazepines. Benzodiazepines bind to the
GABA-A receptor. This receptor is made up of five subunits, e.g.,
alpha, beta, gamma, delta, epsilon, rho, etc. A common GABA-A
receptor found in the CNS is made up of twoalpha-1 subunits, two
beta-2subunits and one gamma-2subunit.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 30-60mins 1-2hrs 3hrs
IM 15-30mins 30-45mins 3hrs
IV 1-5mins 30mins 15-60mins
RECTAL rapid 1.5hr 3hrs

Half time: 20-80 hours

Adverse effect:
 Drowsiness, tiredness, dizziness, sleep problems
(insomnia), memory problems, poor balance or
coordination, slurred speech, trouble concentrating,
irritability, diarrhea, constipation, increased sweating,
headache, nausea, vomiting, upset stomach, blurred vision,
apetite or weight changes, swelling of hands or feet, muscle
weakness, dry mouth, stuffy nose, loss of interest in sex.
Generic name: PHENOBARBITAL

Indications: Sedative. Treatment of generalized tonic-clonic and


cortical focal seizures. Emergency control of certain acute seizures
(associated with meningitis).

Actions: General CNS depressant; barbiturates inhibit impulse


conduction in the ascending RAS, depress the cerebral cortex, alter
cerebellar function, depress motor output, and can produce
excitation, sedation, hypnosis, anesthesia, and deep coma.

Pharmacokinetics:
Route Onset Peak Duration
ORAL 15mins 30-60mins 10-16hrs
IM, unknown 10-30mins 4-6hrs
SUBCUTANEOUS
IV 10-15mins 5mins 4-6hrs

Half time: 79 hours

Adverse effect:

CNS: drowsiness, somnolence, lethargy, ataxia,vertigo, “hangover”


feeling, thinking abnormalities, paradoxical excitement, anxiety,
hallucinations

CV: bradycardia, hypotension, syncope

Respiratory: serious hypoventilation, respiratory depression

Hypersensitivity reactions: rash, serum sickness, Steven-Johnson


syndrome Development of physical tolerance and psychological
dependence
Generic name: AMITRIPYLINE

Indications: This drug in indicated for the following conditions:


Major depressive disorder in adults, Management of neuropathic
pain in adults, Prophylactic treatment of chronic tension-type
headache (CTTH) in adults, Prophylactic treatment of migraine in
adults.

Actions: Inhibits the membrane pump mechanism responsible for


the re-uptake of transmitter amines, such as norepinephrine and
serotonin, thereby increasing their concentration at the synaptic
clefts of the brain.

Pharmacokinetics:
Route Onset Peak Duration
ORAL varies 2-4hrs unknown

Half time: 8-16 hours

Adverse effect:

CV: orthostatic hypotension, hypertension, arrhythmias,


palpitations, myocardial infarction, angina, stroke

GI: dry mouth, constipation, nausea, vomiting, anorexia, increased


salivation, cramps, diarrhea

GU: urinary retention and hesitancy, loss of libido, changes in


sexual functioning

Miscellaneous: alopecia, weight gain or loss, flushing, chills, nasal


congestion Abrupt cessation causes withdrawal syndrome
characterized by nausea, headache, vertigo, malaise, and nightmares
Generic name: CLOZAPINE

Indications: Primary indications for clozapine in patients with


schizophrenia or schizoaffective disorder are schizophrenia
symptoms partially or fully resistant to treatment with other
antipsychotic drugs, or accompanied by persistent suicidal or
self-injurious behavior.

Actions: Clozapine's antipsychotic action is likely mediated through


a combination of antogistic effects at D2 receptors in the
mesolimbic pathway and 5-HT2A receptors in the frontal cortex. D2
antagonism relieves positive symptoms while 5- HT2A antagonism
alleviates negative symptoms.

Pharmacokinetics:
Route Onset Peak Duration
ORAL varies 1-6hrs Weeks

Half time: 4-12 hours

Adverse effect:
 drowsiness, blurred vision, convulsions (seizures), or to
have trouble with thinking or controlling body movements,
which may lead to falls, fractures or other injuries

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