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Lecture 17 Introduction to parenteral

The document provides an overview of parenteral dosage forms, specifically injections, which are sterile preparations intended for administration via injectable routes. It details various parenteral routes including intravenous, intramuscular, subcutaneous, intradermal, intraspinal, and intra-articular, highlighting their applications, advantages, and potential risks. The importance of maintaining sterility and the rapid action of drugs administered parenterally, especially in emergencies, is emphasized.

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Aqib Malik
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2 views

Lecture 17 Introduction to parenteral

The document provides an overview of parenteral dosage forms, specifically injections, which are sterile preparations intended for administration via injectable routes. It details various parenteral routes including intravenous, intramuscular, subcutaneous, intradermal, intraspinal, and intra-articular, highlighting their applications, advantages, and potential risks. The importance of maintaining sterility and the rapid action of drugs administered parenterally, especially in emergencies, is emphasized.

Uploaded by

Aqib Malik
Copyright
© © All Rights Reserved
Available Formats
Download as PDF, TXT or read online on Scribd
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Introduction to Parenteral

dosage form
Kamran Hidayat
1.1. Injections
Injections are sterile, pyrogen-free (endotoxin) preparations intended to be
administered parenterally.
The term parenteral refers to the injectable routes of administration. It derives from the
Greek words para(outside) and enteron(intestine) and denotes routes of administration
other than the oral route.

Pyrogens, or bacterial endotoxins, are organic metabolic products shed from gram
negative bacteria, which can cause fever and hypotension in patients when they are
in excessive amounts in intravenous (IV) injections.

Parenteral routes are used


when rapid drug action is desired, as in emergencies;
when the patient is uncooperative, unconscious, or unable to accept or tolerate oral
medication;
or when the drug itself is ineffective by other routes
With the exception of insulin injections, which are commonly self-administered by
diabetics, most injections are administered by the physician, physician’s assistant, or
nurse in the course of medical treatment.

Perhaps the earliest injectable drug to receive official recognition was the hypodermic
morphine solution, which appeared first in the 1874 addendum to the 1867 British
Pharmacopeia and, in 1888, in the first edition of the National Formulary (NF)of the
United States.

Today, literally hundreds of drugs and drug products are available for parenteral
administration.
1.1. Parenteral Routes of Administration
Drugs may be injected into almost any organ or area of the body, including the joints
(intraarticular), joint fluid area (intrasynovial), spinal column (intraspinal), spinal fluid
(intrathecal), arteries (intra-arterial), and, in an emergency, even the heart
(intracardiac).

However, most injections go


into a vein (intravenous, IV),
into a muscle (intramuscular, IM),
into the skin (intradermal, ID; intracutaneous),
or under the skin (subcutaneous, SC).
i. Intravenous Route
Intravenous injections and infusions are administered into an easily accessible
prominent vein near the surface of the skin.
The volumes administered can range from 1 mL for an intravenous injection up to
several litres for an intravenous infusion.
Drug solutions at high or low pH or highly concentrated hypertonic solutions will
damage the cells lining the vein and cause localized pain and inflammation
(thrombophlebitis).
Injections which are
formulated either as water-in-oil emulsions or suspensions must not be administered by
the intravenous route. This is because the suspended drug particles can physically
block blood capillaries and oil of of a water-in-oil injection could cause a fat
embolism, again blocking blood vessels.
IV drugs provide rapid action compared with other routes of administration, and
because drug absorption is not a factor, optimum blood levels may be achieved with
accuracy and immediacy not possible by other routes.
In emergencies, IV administration of a drug may be lifesaving because of the
placement of the drug directly into the circulation and the prompt action that ensues.

On the negative side, once a drug is administered intravenously, it cannot be retrieved.


In the case of an adverse reaction to the drug, for instance, the drug cannot be easily
removed from the circulation, as it could, for example, by induction of vomiting after
oral administration of the same drug.
Strict aseptic precautions must be taken at all times to avoid the risk of infection.
Not only are the injectable solutions sterile, the syringes and needles must also be
sterilized.

Both small and large volumes of drug solutions may be administered intravenously. The
use of 1,000-mL containers of solutions for IV infusion is commonplace in the hospital. The
infusion or flow rate may be adjusted according to the needs of the patient. Generally,
flow rates for IV fluids are expressed in milliliters per hour and range from 42 to 150 mL/h.

The main hazard of IV infusion is thrombus formation induced by the catheter or needle
touching the wall of the vein. Thrombi are most likely when the infusion solution is
irritating to the biologic tissues. A thrombus is a blood clot formed within the blood vessel
(or heart), usually because of slowing of the circulation or an alteration of the blood or
vessel wall.

Once such a clot circulates, it becomes an embolus, carried by the blood stream until it
lodges in a blood vessel, obstructing it and resulting in a block or occlusion referred to as
an embolism.
IV drugs ordinarily must be in aqueous solution; they must mix with the circulating blood
and not precipitate from solution.

ii. Intramuscular Route


Intramuscular injections are preferably administered into the tissue of a relaxed muscle.
The muscle sites commonly used for intramuscular injection are the buttock, thigh or
shoulder muscles
IM injections of drugs provide effects that are less rapid but generally longer lasting than
those obtained from IV administration.
Aqueous or oleaginous solutions or suspensions of drug substances may be administered
intramuscularly in volumes of up to 4 mL.

Drugs in solution are more rapidly absorbed than those in suspension, and oleaginous
preparations.
IM injections are performed deep into the skeletal muscles. The point of injection should
be as far as possible from major nerves and blood vessels.
Injuries to patients from IM injection usually are related to the point at which the needle
entered and where the medication was deposited. Such injuries include paralysis
resulting from neural damage, abscess (mass filled with pus caused due to infection.), cyst
(abnormal sac in the body filled with fluid) , embolism, hematoma (solid swelling of clotted
blood within the tissues).

iii. Subcutaneous Route


Subcutaneous (also called hypodermic) injections are administered into the loose
connective and adipose tissues immediately beneath the dermal skin layer.
The SC route may be used for injection of small amounts of medication. Injection of a
drug beneath the skin is usually made in the loose interstitial tissue of the outer upper
arm, the anterior thigh, or the lower abdomen.
As this tissue is highly vascular, drugs administered by the subcutaneous route are fairly
rapidly and predictably absorbed from this site.
A common example of a drug administered by
subcutaneous injection is insulin.
The maximum amount of medication that can be
comfortably injected subcutaneously is about 1.3 mL,
and amounts greater than 2 mL will most likely cause
painful pressure.
iv. Intradermal injections
Intradermal injections are given into the skin between
the epidermal and dermal layers.
Volume of up to 0.2 mL can be given by this route, and
absorption from the intradermal injection site is slow.
This route is used for immunological diagnostic tests,
such as allergy tests, or the injection of tuberculin
protein to determine immunity against tuberculosis.
v. Intraspinal injections are given between the vertebrae of the spine into the area
of the spinal column. Only drugs in aqueous solution are administered by this route.
Intrathecal injections are administered into the cerebrospinal fluid (CSF). This route
can be used for spinal anaesthesia.
Intrathecal injections are also given to introduce drug substances into the CSF that
would otherwise not diffuse across the blood–brain barrier. Typically, these could
be antibiotics to treat meningitis, or anticancer agents such as methotrexate or
cytarabine.
Volumes up to 10 mL can be administered by intrathecal injection

vi. Intra-articular injections


Intra-articular injections are given into the synovial fluid of joint cavities such as the
knee. Aqueous solutions or suspensions can be administered by this route. This route
of injection produces a local effect, and typically anti-inflammatory drugs are
administered to treat arthritic conditions or sports injuries.
Thanks

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