Assigned by: Mr.
AbdulRaheem
Submitted by: Saba Ismail
Activity 17
PREPARE DRUG PROFILE OF
Adrenlaine
Drug Category (PRESCRIPTION/OTC):
Prescription
WHO Essential Drug List: Present
National Essential Drug List: Present
1. PRODUCT DESCRIPTION
SR Brand Name Manufacturer Dosage Strength Pack Size Price/U
No Form nit
1 Adecaine P.D.H Injection Lignocaine:20mg/ 2ml×100s 250.00
With pharmaceuticals ml rs/
adrenaline (PVT)LTD. Adrenaline:0.001
% w/v
2 Adrenaline Venus Pharma Injection 1mg/ml 10ml 11.52rs
1ml×100s 158.75r
25ml s/
21.0rs/
3 L-caine OPHTH Pharma Injection Lignocaine:20mg/ 10ml×50s 950 Rs
(PVT) LTD ml
Adrenaline:0.001
%w/v
4 Medicaine Hospital supply Injection Lignocaine:20mg/ 1.8 676Rs
corporattion ml ml×50carts
Adrenaline:0.001
%w/v
5 MB-CAIN Multinational Injection Lignocaine:20mg/ 10ml×50s 650Rs
business link ml
Adrenaline:0.001
%w/v
How to store this drug (instructions for patients)
❏ Store between 20° to 25°C (68° to 77°F) .
❏ Epinephrine is light sensitive. Protect from light and freezing.
❏ Inspect visually for particulate matter and discoloration prior to administration.
❏ Do not use the solution if it is colored or cloudy, or if it contains particulate matter.
2. CHEMISTRY OF DRUG
Chemical Class: Catecholamines(sympathomimetic monoamine derived from the amino acids
phenylalanine and tyrosine)
Chemical Nature/Structure:
1,2-Benzenediol, 4-[(1R)-1-hydroxy-2-(methylamino)ethyl]-
Chemical Formula: C₉H₁₃NO₃
Physical Properties:
White to nearly-white microcrystalline powder or granules.
Odor:Odorless.
Melting point 211-212°C or (412 to 414 ° F)
Aqueous solutions are slightly alkaline.
Taste:Slightly bitter, numbing taste.
Colour:
Brown (in air)
Light brown or nearly white crystalline powder
Minute crystals, gradually browning on exposure to liaght and air
Colorless microcrystals
Stability/shelf life: In some commercially available injections, the air has been replaced with nitrogen to
avoid oxidation. Withdrawal of doses from multiple-dose vials introduces air into the vials, subjecting the
remaining epinephrine to oxidation. Oxidation of the drug imparts first a pink, then a brown color;
epinephrine preparations must not be used if they have a pinkish or darker than slightly yellow color or
contain a precipitate.
Specific optical rotation :-50 deg to -53.3 deg at 25 °C/D (in 0.6N HCl)
Water Solubility: In water, 180 mg/L at 20 °C
Very slightly soluble in alcohol. Readily soluble in aqueous solutions of mineral acids, NaOH, and KOH.
Insoluble in aqueous solutions of ammonia and of the alkali carbonates. Insoluble in chloroform, ether,
acetone, oils.
Molecular Weight: 183.21 (NTP, 1992)
3. PHARMACOKINETICS
1). ABSORPTION:
Adrenaline has a rapid onset of action after intramuscular administration and in the shocked patient its
absorption from the intramuscular site is faster and more reliable than from the subcutaneous site. The
plasma half-life is about 2-3 minutes. However, when given by subcutaneous or intramuscular injection,
local vasoconstriction may delay absorption so that the effects may last longer than the halftissuesuggests.
2). DISTRIBUTION
Bio- Protein Placental Blood Secreted In Volume Time For
Availability Binding Barrier Brain Milk Of Onset Of
(%) Barrier Distribution Action
Following I.V 15–20% Can cross Can't cross Not exactly the apparent Rapid
& IM route known. volume of onset of
,bioavailabilit Some distribution is action in
y=100% studies 2.0-1.5 L/kg. case of
Oral shows that IV/IM
absorption is it may SC
75% ±5. secretes. administrat
ion during
asthmatic
attack
3). ELIMINATION
Half LIFE Site Of Metabolism Active Metabolite Route Of Excretion
(if any)
After IV infusion Mainly Liver (& Metanephrine Urine
Half life is 5 to 10 tissues)
minutes.
4. CLINICAL PHARMACOLOGY
Pharmacological Class Sympathomimetic
Catecholamine
Therapeutic class Beta-adrenergic agonist
Mechanism Of Action Adrenlaine acts on alpha and beta-adrenergic receptors. Adrenlaine
acts on alpha and beta receptors and is the strongest alpha receptor
activator . Through its action on alpha-adrenergic receptors,
epinephrine minimizes the vasodilation and increased the vascular
permeability that occurs during anaphylaxis, which can cause the
loss of intravascular fluid volume as well as hypotension.
Epinephrine relaxes the smooth muscle of the bronchi and iris and is
a histamine antagonist, rendering it useful in treating the
manifestations of allergic reactions and associated conditions. This
drug also produces an increase in blood sugar and increases
glycogenolysis in the liver. Through its action on beta-adrenergic
receptors, epinephrine leads to bronchial smooth muscle relaxation
that helps to relieve bronchospasm, wheezing, and dyspnea that may
occur during anaphylaxis.
Spectrum (in Nill
case of antibiotic)
Contradictions Epinephrine is contraindicated in patients with known
hypersensitivity to sympathomimetic amines, angle closure
glaucoma, and in nonanaphylactic shock.
Adrenaline should not be used during labour or, with local
anaesthesia of peripheral structures including digits and ear lobe.
Use in the presence of ventricular fibrillation, cardiac dilatation,
coronary insufficiency, organic brain disease or atherosclerosis,
except in emergencies where the potential benefit clearly outweighs
the risk.
Precautions Adrenaline should be used with caution in patients with
hyperthyroidism, diabetes mellitus, phaeochromocytoma, narrow
angle glaucoma, hypokalaemia, hypercalcaemia, severe renal
impairment, prostatic adenoma leading to residual urine,
cerebrovascular disease, organic brain damage or arteriosclerosis, in
elderly patients, in patients with shock (other than anaphylactic
shock) and in organic heart disease or cardiac dilatation (severe
angina pectoris, obstructive cardiomyopathy, hypertension) as well
as most patients with arrhythmias. Anginal pain may be induced
when coronary insufficiency is present.
Repeat administration may produce local necrosis at the sites of
injection.
Prolonged administration may produce metabolic acidosis, renal
necrosis and adrenaline fastness or tachyphylaxis.
Adrenaline should be avoided or used with extreme caution in
patients undergoing anaesthesia with halothane or other halogenated
anaesthetics, in view of the risk of inducing ventricular fibrillation.
Do not mix with other agents unless compatibility is known.
Adrenaline should not be used during the second stage of labour.
Accidental intravascular injection may result in cerebral
haemorrhage due to the sudden rise in blood pressure.
Adrenaline 1 in 1000 should not be diluted to 1 in 10,000 for use in
cardiac resuscitation - when the 1 in 10,000 strength of adrenaline is
required for this indication a “ready to use” preparation should be
selected.
Monitor the patient as soon as possible (pulse, blood pressure, ECG,
pulse oximetry) in order to assess the response to adrenaline.
The best site for IM injection is the anterolateral aspect of the middle
third of the thigh. The needle used for injection needs to be
sufficiently long to ensure that the adrenaline is injected into muscle.
Intramuscular injections of Adrenaline into the buttocks should be
avoided because of the risk of tissue necrosis
FDA Pregnancy Class Adrenaline has been assigned to pregnancy category C by the FDA.
Clinically Monitoring Parameters
Heart rate, blood pressure (invasive blood pressure monitoring recommended while receiving continuous
infusion); monitor site of infusion for blanching/extravasation; continuous cardiac monitoring required
during continuous infusion. If using to treat hypotension, assess intravascular volume prior to and during
therapy; support as needed; monitor for cardiac arrhythmias, hyperlactatemia, and hyperglycemia.
Consult individual institutional policies and procedures.
5. DOSAGE SCHEDULE
Indications Route Of Recommended Dosage Duration Of
Administration Therapy (if any)
Anaphylaxis intramuscularly 0.1 mg/kg of 0.5 mg Repeated after 5 to
(IM), intravenously 1mg/ml (Adult) 10 minutes
(IV) 0.3 mg
(Child)
Cardiac arrest Intravenously 0.5 -1 mg 1mg Every 3 to 5
minutes
Hypotensive Intravenously 0.05-2 adjust dose q10-15
With septic shock mcg/kg/minute IV min by 0.05-0.2
mcg/kg/minute
6. ADJUSTMENT OF DOSAGE (if required) HEPATIC/RENAL
IMPAIRMENT
Renal impairment requires monitoring as adrenaline causes renal blood vessel
constriction and can decrease urine impairment. In patients with chronic kidney disease
(CKD) and various other renal pathologies and in hepatic disorders, clinical judgment is
necessary.
7. SIDEEEFFECT
These are following side effects:
anxiety, apprehensiveness, restlessness, tremor, weakness, dizziness, sweating, palpitations, pallor, nausea
and vomiting, headache, and respiratory difficulties. These symptoms occur in some persons receiving
therapeutic doses of epinephrine, but are more likely to occur in patients with heart disease, hypertension,
or hyperthyroidism .
8. ADMINISTRATION GUIDELINES
1) FOR ORAL USE
How to take this drug?
Given orally, epinephrine will rapidly degrade in the GI tract and is not absorbed at all.
Can you break or crush tablet?
No.
2) INSTRUCTIONS FOR TOPICAL USE (IF ANY)
Apply solutions topically as a spray or on cotton or gauze to the skin, mucous membranes, or other
tissues.
3) For I/V ROUTE
IV Bolus, Rate Of Administration Administer slowly (after appropriate dilution) by
IV injection or continuous IV infusion
Solvent For Reconstitution 1:1000 with 9 mL normal salinefor injection.
(for dry powder for injection)
Volume To Be Added/ Concentration 1mL
Temperature And Storage Time After Store at room temperature (25°C) or refrigeration
Reconstitution (4°C) is 24 hr
Compatible IV Fluids ● Sodium chloride 0.9%
● Sodium lactate 1/6 M
● Dextrose–Ringer’s injection combinations
● Dextrose–Ringer’s injection, lactated,
combinations
● Dextrose 5% in Ringer’s injection, lactated
● Dextrose–saline combinations
● Dextrose 5% in sodium chloride 0.9%
● Dextrose 2.5, 5, or 10% in water
Pharmaceutical Incompatibilities Ampicillin sodium
Aminophylline
Hydroxyethyl starch 130/0.4 in sodium chloride
0.9%
Micafungin sodium
Infusion Rate Continuous infusion
● low rates (e.g., <0.3 mcg/kg per minute)
generally produce predominantly β-
adrenergic effects
● higher rates (e.g., >0.3 mcg/kg per minute)
produce α-adrenergic vasoconstriction.
Till condition becomes better.
9. DRUG—DRUG INTERACTIONS
Interacting Drug Severity Mechanism Outcome Managem
ent
Antidiabetic Moderate Epinephrine induces Epinephrine causes a May
agents (e.g., increases in plasma prompt increase in require
insulin, oral levels of glucagon, a blood glucose increased
hypoglycemics) lipolytic and concentration in the antidiabeti
hyperglycemic postabsorptive state, c dosage.
hormone. This effect is me-
● Because diated by a transient
● it increases increase in hepatic
glycogenolysi glucose production and
s in the liver an inhibition of glucose
(Beta 2 disposal by insulin-
effect). dependent tissues.
● Increased
release of
glucagon
(Beta 2 effect)
● Decreased
release of
insulin (alpha
2 effect)
These mechanism are
mediated via the
cAMP
Mechanism.
Digoxin Moderate The concomitant use Using digoxin together Caution
of sympathomimetic with EPINEPHrine should be
agents and cardiac may occasionally cause exercised
glycosides may an irregular heart if these
increase the risk of rhythm. two drugs
cardiac arrhythmias. are
The mechanism of this coadminis
interaction is not Increased tered.
known cardiosensitivity to Electrocar
epinephrine. diogram
monitorin
g (ECG) is
recommen
ded. The
use of
epinephrin
e
(adrenalin
e) with
high doses
of digitalis
glycosides
is not
recommen
ded.
Propranolol Major Beta-blockers like Antagonism of cardiac Avoid
propranolol may and bronchodilating taking
reduce the effects of effects. these
epinephrine. May potentiate pressor medicatio
It works by blocking effects of epinephrine. ns
the effects of the It cause your blood together.
hormone epinephrine, pressure to be
also known as increased. Your heart
adrenaline. rate may slow down.
Anesthetics, Major Increased This can cause Use with
general (e.g., cardiosensitivity to symptoms of irregular caution, if
halogenated epinephrine. heartbeat, chest at all;
hydrocarbons tightness, blurred increased
[e.g., halothane], vision, nausea, and risk of
cyclopropane) seizures. ventricular
arrhythmi
as such as
VPCs,
VT, or
VF;
contraindi
cated with
chlorofor
m,
trichloroet
hylene, or
cycloprop
anea
May not
be
absorbed
rapidly
enough
with
topical
hemostatic
use to
present a
problem in
short
procedure
sa
10. DRUG FOOD INTERACTION
Food Nature Of Interaction
No such food is found
11. DRUG—LAB INTERACTIONS
Lab Test Nature Of Interaction
No such interaction
12. TOXICOLOGY
Toxic Dose Sign & Symptoms Of Toxicity Management/Treatment
(including antidote)
Its toxicity is usually caused by Tremor Phentolamine reversed
iatrogenic errors. Prespiration epinephrine injection after 1 hour
● For CPR, (greater than 1 Weakness 25 minutes.
mg/dose) Dizziness
● For anaphylaxis, greater Palpitations
than 0.5 mg/dose . Pallor
● For bronchospasm,
Greater than 0.5 mg/dose).
In overdose there is a typical
rapid onset of agitation,
hypertension, tachycardia, and
dysrhythmias.
