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Terms in this set (30)
what is the common reason for using parenteral formulations
Control onset/ concentration and eliminations
Biological effect not possible orally - poor absorption and/or degradation
Unconscious, uncooperative eg narcotic abuse, tonic-clonic (grand mal) seizures, psychotics etc.
Compliance eg depot injections for mental illness.
Local effect such as anaesthetics eg dental treatment.
can suspensions or emulsions be given as IV
yes they can
what is a co-solvent
secondary solvent used to increase or enhance solubility of the solid
eg eg glycerin, ethanol, propylene glycol, polyethylene glycol
are hypertonic solutions possible using injections
only via SLOW administration via IV
not ID SC IM
what must you add to hypertonic solutions to adjust for tonicity
NaCl, KCL, dextrose
IM is less rapid and has a longer duration than _____
but is more rapid than?
so what is the order
so it goes IV fastest IM then SC slowest
why would you prefer to inject into deltoid arm muscle over thigh or buttocks
higher blood flow at arm due to higher vascularity and higher fat content
age and disease affect blood flow
higher blood flow = high absorptions
when would you use SC
when its a small volume
self medication as lack of infection issue
what drugs can you use SC for
Poorly absorbed and fragile drugs and typically water soluble and non irritating
IP what is it and whens it used
Intraperitoneal = cavisity .organ
liver kidney bladder
used in chemo for abdo tumours
dialysis in renal failure
better in small lipid soluble drugs
needle free injectors
spring powered - though sands of uses
high pressure gas forces drug through skin
gas burst acceleration of powdered drug particles to________ speeds
what kind of drugs can this be used for
needs to be potent as only small amount of drug can be administered
-->increase skin permeability by creating micron-scale pathways in skin,
-->actively drive drugs into the skin during microneedle insertion,
-->target to the stratum corneum, although microneedles typically pierce across the epidermis &into the superficial dermis too.
Transdermal delivery is limited due to the significant barrier to penetration across the skin ,which is associated primarily with the outermost ________ layer of the epidermis.
daily dose of drug that can be delivered from a transdermal patch is typically _______mg
-->limiting this route of administration to ______
Formulation penetration enhancement in creams, gels and patches, through either or both of:
drug and delivery vehicle,
modification of stratum corneum.
Powered penetration enhancement devices such as:
iontophoresis, phonphoresis & electroporation patches
3 transdermal penetration routes
1. Directly across the stratum corneum
Shunt or appendage routes:
2. through the sweat ducts,
3.via the hair follicles and sebaceous glands
The majority of skin penetration enhancement has focused on___________across the stratum corneum.
Appendages comprise small area for permeation (~ 0.1%), contribution to steady state flux of most drugs is minimal, except:
iontophoretic drug delivery primarily via the shunt routes as less electrical resistance.
Brick & mortar' structure
layers of keratin-rich corneocytes = bricks
intercellular lipid matrix = mortar
Water is essential as a _____ to prevent cracking of the stratum corneum
Intercellular route is the main pathway for most drugs
true or false
soluble in the lipid regions or in formulations disrupting the lipid regions
more hydrophilic drugs penetrating aqueous regions of keratin filaments, BUT must also travel across intercellular lipid region
Solubility and partition coefficient affect drug diffusion
-->intermediate partition coefficients - log P octanol/water of 1-3
-->adequate solubility within the lipid domains of the stratum corneum to permit diffusion through this domain,
-->sufficient hydrophilic nature to allow partitioning into the viable tissues of the epidermis.
Skin permeation enhancement
3)Ion pairs, complexes
perferable characteristics of drug
eg mol wt
low molecular size (< 500 Da) as higher diffusion, low melting point (re. Solubility)
where a drug does not possess ideal physicochemical properties, manipulation of the stratum corneum to enhance diffusion becomes necessary.
3)Bypass / removal
4)Powered electrical devices:
Drug vehicle: prodrug design
Pro-moiety increases ________ hence increases solubility and transport of the parent drug in the stratum corneum.
_____ in viable epidermis release parent drug by _______, optimising solubility in the aqueous epidermis.
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