Exam 2: Parenteral

Parenteral Products

dosage forms administered as injections

T/F: Injections do NOT bypass normal body defense mechanisms

False

Free from substances that cause fever (ex. Endotoxins)

Nonpyrogenic

Free of any living microorganisms (bacteria, viruses, fungi, spores) 

Sterile

T/F: Parenteral products only need to be sterile

False; & Non-pyrogenic

Intracutaneous; between the dermis and epidermis

Intradermal

Volume that can be injected intradermally

0.1 - 0.2 mL

Intradermal has (good/poor) vascularity?

poor

Hypodermic; injections under the skin and into the tissue

Subcutaneous

What types of suspensions are NOT suitable for Subcutaneous injections due to pain and irritation?

Aqueous and Oily

Why are Subcutaneous injections popular?

Convenient

Injection made into muscle tissue with the skin, subcut tissue, and membrane enclosing the muscle

Intramuscular 

T/F: Intramuscular routes can administer aqueous/oily suspensions and oily solutions 

True 

Suspensions and Oil can cause what if administered Intravenously?

Block blood vessels

Injections directly into the veins

Intravenous

What ONLY type of solution can be used for Intravenous administration?

Aqueous

Intracardiac 

injections directly into the heart muscles or ventricles

When is intracardiac and intraspinal administration used?

Emergencies (ex. cardiac failure) or cannot use other methods

What cardiac stimulants are used for intracardiac administration?

Adrenaline (epinephrine) or Isoprenaline

Intraspinal

parenteral administration into and around the spinal cord

The intraspinal injection must have what same measure as cerebral-spinal fluid?

Density

What sub-category of an intraspinal injection are made into the cerebral-spinal fluid surrounding the spinal cord? (Ex. Spinal anesthetics, Streptomycin for tubular meningitis)

Intrathecal or Subarachnoid injection

What sub-category of an intraspinal injection are made between the dura mater and the inner vertebrae?

Peridural injections

T/F: anyone can do an intracardiac and intraspinal injection

False; experts only

Solution preparations that are ready for administration

Injection

Dry solids in addition to suitable vehicles that yield solutions conforming in all aspects to the requirement for injection

For Injection

Liquid preparation of drug substance dissolved or dispersed in a suitable emulsion

Injectable Emulsion

Liquid preparation of solid suspended in a suitable liquid medium

Injectable Suspension

Dry solid in addition of suitable vehicle that yields preparation conforming in all respect to the requirement of an injectable suspension

For Injectable Suspension

Critical factors for Parenteral product formulation

Vehicle for drug to be dissolved or dispersed
Volume of injection
Osmotic pressure
pH adjustment
Stabilizers
Preservatives
Sterility
Pyrogen free

When are preservatives needed when formulating injections

Multi-dose 

What 2 qualities does a drug vehicle must have

Pharmacologically inert 
Non-toxic

What is the ideal vehicle for most injections due to its compatible tolerance with the body?

Water

What conditions can result in the replacement of water as the drug vehicle 

Drug is prone to hydrolysis (breaks esters) 
Poorly water soluble drugs 
When depot effect is needed (oily vehicles like Progesterone0

what type of water is used for injections

sterilized distilled water from pyrogen 

What are considered thermostable, water soluble, and unaffected by bactericides and cannot be removed via sterilization?

Pyrogens

How are pyrogens can be removed through what process due to being non-volatile?

Distillation

Single, quick (1 minute) concentrated amount of a drug, fluid, or other substance to raise its concentration to an effective level quickly

Bolus Dose

A Bolus Dose must be less than what amount?

10 mL

What type of parenteral administration uses more than 10 mL?

IV Infusion

What is the accepted condition for an o/w emulsion to be administered intravenously

Globular size is controlled

T/F: w/o can be administered through IV

False

T/F: Co-solvents can be used as vehicles

True

Co-solvents are added to water to improve what?

Solubility

What are used when medications cannot dissolved in water for injections?

Co-solvents

Examples of Co-solvents

Glycerol
Propylene Glycol Benzyl Alcohols
PEG
Ethanol

Ethanol is (first/last) option as a co-solvent

Last

T/F: Ethanol causes pain and tissue damage

True

What is the effect that results in a slow release?

Depot Effect

An injection’s volume is dependent on what? 

Medication solubility & route of administration

Intracutaneous injections have small volumes to prevent what?

Blisters

T/F: Some injections need to be isotonic with plasma

True

Solutions with lower Osmotic Pressure than blood is considered to be…

Hypotonic

Solutions with higher Osmotic Pressure than blood are considered to be…

Hypertonic

What are BOTH Hypotonic and Hypertonic termed as?

Paratonic

Blood cells undergo hemolysis in what type of solutions?

Hypotonic

Blood cells that shrink as water passes outward from the cell in what type of solutions?

Hypertonic

What is another name for a hypertonic effect?

Crenation

T/F: Blood cell shrinkage and Hemolysis is reversible

False; only shrinkage

What type of tonicity must IV injections be due to direct blood contact?

Isotonic

What type of tonicity must Intrathecal injections must be due to CSF’s paratonic solution?

Isotonic 

T/F: Intrathecal can be paratonic 

False; causes headache and vomiting 

What type of tonicity must Subcutaneous injections be to reduce pain?

Isotonic 

What is used to adjust pH levels

Buffer

Why might pH levels need to be adjusted?

Increase stability & solubility of the actives
Minimize pain, irritation, & necrosis
Prevent microorganisms growth

What pH levels prevent microorganism growth for injections

8-9

What type of stabilizers added to injections help reduce oxidation rates of drugs when in aqueous systems?

Antioxidants 

Examples of Antioxidants (Sulphorous Acid Salts)

Sodium Bisulfite
Sodium Metabisulfite
Sodium Sulfite

What stabilizer can replace air in the final container to prevent decomposition from oxygen?

Nitrogen

T/F: injections are sterilized in the final container to minimize possible contamination

True

Methods of Sterilization

Dry heat for oily injections
Autoclaving for thermostable aqueous preps
Heat with bactericide for injections thermolabile to autoclaving
Filteration for dry heat alternative

People who are not compatible with sulfur can develop what?

Steven Johnsons Syndrome

People with Steven Johnsons Syndrome cannot use what?

Antioxidants

T/F: Autoclaving has water

True

Which sterilization process has neither water and heat

Filteration