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106 Cards in this Set
- Front
- Back
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Name as many mucosal routes of administration as possible
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Ocular, nasal, buccal, gingival, sublingual, pulmonary, rectal, vaginal
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What is the pharmacy definition of parenteral?
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IV
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What is the literal definition of parenteral?
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Outside the intestine
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What are the four types of parenteral delivery?
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Intradermal, subcutaneous, intramuscular, intravenous
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Typical uses for intradermal delivery?
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Diagnostic measurement, allergy testing, vaccination
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Features of intradermal delivery?
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0.1-0.2mL volume, 1.5-2mm deep, high variation in delivery (inconsistent)
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What is an IV bolus?
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Single rapid (up to 2min) small volume (<1mL) injection
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Why does IM have more variation than IV?
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IM requires absorption step - variation between patients and sites
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Which parenteral delivery penetrates the deepest?
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IM
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Typical volume of injection for ID?
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0.1-0.2mL
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Typical volume of injection for SC?
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<1mL
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Typical volume of injection for IM?
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<2-4mL
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Typical volume of injection for IV?
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<1mL up to 500mL
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Which parenteral delivery method has a volume of 0.1-0.2mL?
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ID
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Which parenteral delivery method has a volume of <1mL?
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SC
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Which parenteral delivery method has a volume of 2-4mL?
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IM
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What the the main factor that affects the difference in absorption between SC and IM?
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Blood flow
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Which has generally slower absorption, SC or IM?
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SC
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What are the three main sites for IM in order of decreasing absorption rate?
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Arm (deltoid) > thigh (vastus lateralis) > buttock (gluteus maximus)
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Which muscle is used for IM in the arm?
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Deltoid
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Which muscle is used for IM in the thigh?
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Vastus lateralis
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Which muscle is used for IM in the buttock?
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Gluteus maximus
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Three ways to increase blood flow to an injection site?
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Local heating, massage, exercise
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What predetermined, unchangable factor affects absorption through IM?
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Gender, male absorption rate > female
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What differences are there between males and females in the deltoid muscle?
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Females have a thicker deltoid fat pad
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Why are different needles recommended for male/female IM/SC injections?
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Females have a thicker fat pad affecting target depth
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What can be added to (or injected before) SC and IM injections to decrease tissue viscosity?
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Hyaluronidase
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How does hyaluronidase affect SC and IM injections?
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Breaks down connective tissue and decreases tissue viscosity, increasing diffusion
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What relationship is absorption from SC and IM sites?
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First order, dependant on concentration of drug in solution
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What are the two limiting parameters for IM absorption?
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Perfusion limited or device limited
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When does increasing perfusion not increase absorption for IM?
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When the absorption is device limited
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What is the pH of skeletal muscle?
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~6
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How does partitioning affect IM injections?
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Acidic pH shift on injection can cause ppt to form, which may be absorbed slowly (and erratically), may cause pain
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How does drug lipophilicity affect IM absorption?
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More lipophilic drugs don't partition well into ECF, poorly absorbed
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How does molecular weight affect IM absorption?
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Larger molecules over 1000 daltons give progressively slower absorption rates
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Why does alprenolol unexpectedly give better absorption compared to similar lipophilic IM drugs?
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Is an irritant, causes inflammation and increases diffusivity of tissue
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What are the four drug properties that affect IM/SC absorption?
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Concentration, ionisation (solubility, partitioning), lipophilicity, molecular weight
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What is drug targetting?
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An increased accumulation of drug in the required area of the body compared to other tissues/organs
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Why are some chemo drugs given by IV?
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Better control of plasma level to improve delivery to target site, and improve efficacy and safety of narrow therapeutic range drugs
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What are the four main nano-medicine delivery methods?
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Liposomes, drug/polymer conjugates, micelles, nano particles
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What is EPR?
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Enhanced permeation and retention effect, where tumors cause certain sized molecules to accumulate
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What is the RES?
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Reticuloendothelial system, phagocytic immune cells that engulf foreign particles and infectious agents
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How does PEGylated liposomal doxorubicin improve delivery?
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Binds water and "hides" liposome from reticuloendothelial system
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What is active drug targetting?
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Targetting molecules specifically bind to a receptor/molecule which is highly expressed on the cancer cell
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What is the difference between PEGylated liposomal doxorubicin and targeted liposomal doxorubicin?
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Targeted molecule targets cells by expressed molecules
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Why use controlled release parenteral devices?
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Increase compliance, reliability, ensure optimal use, control delivery, reduce # administrations: improved disease management
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What are the main administration routes of controlled release parenteral delivery?
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SC and IM
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What can be added to a sustained release parenteral formulation to prolong delivery time?
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Add a vasoconstrictor to the formulation (eg adrenaline)
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Why would adrenaline be added to a sustained release parenteral formulation?
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Vasoconstrictor, prolongs both delivery time and anaesthetic effect
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How is it possible to reduce potential toxicity of an IM injection?
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Add a vasoconstrictor to formulation
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What are some of the typical approaches used in formulation of sustained release parenterals?
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Oily vehicles, aqueous suspensions, emulsions, microparticles, implants
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What affects sustained release with oily vehicles?
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Drug o/w partition coefficient, esp if drug particles must dissolve in the oily phase first
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How can you prolong the release of lipophilic drugs in parenteral release?
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Formulate in an aqueous suspension
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How does a lipophilic drug in an aqueous suspension give an immediate and sustained release?
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Saturated solution gives immediate release, and then suspension particles provide sustained
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What are microparticles, used in parenteral delivery?
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Polymeric microspheres prepared from biodegradable polymers
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Which approach for parenteral formulation can give delivery for months or even years?
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Implantable systems
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What is hemolysis?
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Lysis of red blood cells, loss of membrane integrity
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What can result from free Hb in the circulation?
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Fever, chills, abdominal back pain
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How does hemolysis cause fever, chills, and abdominal back pain?
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Free Hb in circulation
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What can cause hemolysis in parenteral formulations?
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A hypotonic solution, or formulate components interacting with RBC membrane
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What controllable factor of parenteral formulations can affect hemolysis?
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Injection rate
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What are the four parenteral formulation adverse effects?
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Hemolysis, precipitation, phlebitis, and pain
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Where can precipitation occur in parenteral administration?
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At injection site, or downstream from site
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What are the consequences of precipitation in parenteral administration?
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Delayed absorption, endothelial abrasion & phlebitis
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Why does precipitation occur in parenteral administration?
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Drug may be formulated at a different pH to blood, or above solubility in blood
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What is phlebitis?
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Inflammation of the endothelial vein wall due to mechanical or chemical irritation/trauma
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What are the clinical symptoms of phlebitis?
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Pain/burning along vein, redness and warmth, oedema
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What is a serious complication of phlebitis?
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Thrombus formation (thrombophlebitis)
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What can result from parenteral formulation precipitation?
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Deposition on endothelial wall, giving toxicity to those cells, and inflammation
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What is the effective concentration in parenteral IV?
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The formulation conc, multiplied by the factor of inj rate/flow rate
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What is often associated with pain in parenteral IV?
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Phlebitis
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What causes pain in parenteral IV?
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Not understood, often associated with phlebitis
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What approaches can be used to minimise phlebitis?
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Add solubilising agents and stronger buffer capacity, use a slow injection rate, use a large/deep vein
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What approaches can be used to minimise hemolysis?
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Slow injection rate to get rapid dilution, replace hemolytic components with benign
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What can cause pain in IM and SC injections?
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Hydrostatic pressure on surrounding tissue
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What negative outcome can result from irritating drugs and vasoconstrictors in IM and SC injections?
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Abcesses or necrosis
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What factors are considered in choosing pH for parenteral formulation?
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Maximum stability, solubility, and as close to physiological as possible
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What is the tolerable pH range of any IV formulations?
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2 to 12
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Which parenteral administration method can have the widest range of acceptable pH?
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IV
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What is the tolerable range of IV formulations <100mL?
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4 to 10
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What is the tolerable range of IV formulations >100mL?
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6 to 8
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What is the tolerable range of IM & SC formulations?
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3 to 9
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What occurs with IM & SC formulations with a ph < 3?
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Pain
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What occurs with IM & SC formulations with a ph >9?
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Necrosis
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pH range and tonicity allowable in large volume IV formulations?
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6 to 8, must be isotonic.
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What are the two methods usable for sterilising parenteral formulations?
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Terminal sterilisation in packaging, and aseptic processing
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Why would aseptic processing be used in parenteral formulations?
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Instability of the product
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What are the three terminal sterilisation methods for parenteral formulations mentioned?
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Moist heat, dry heat, and radiation
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Which terminal sterilisation method is used for non-aqueous liquids or powders?
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Dry heat
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Which terminal sterilisation method is used for water-wettable materials and aqueous solutions?
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Wet heat
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Which terminal sterilisation method is used for heat sensitive materials and products?
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Radiation
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What are the drawbacks of aseptic processing?
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Lower assurance of sterility, significantly more expensive
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What is intrathecal delivery?
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Delivery directly into the spine
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What are parenteral EUs?
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Endotoxin units
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What is the LAL assay?
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Use of purified, lyophylised horseshow crab blood cells to detect pyrogens
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Why are parenteral formulations lyophylised?
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Increases stability by removed water and lowering hydrolysis
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Advantages of lyophylisation?
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Very low moisture content, can be done aseptically, elegant end product
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Why does a freeze-dried product redisperse rapidly?
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High specific surface area
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What are the three most common diluents in parenteral formulations?
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Water for inj BP, dextrose 5%, normal saline (0.9%)
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Why is the use of ampuoles declining?
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Risk of harm to HCP when opening
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Why is plastic preferred over glass for proteins and peptides?
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Proteins and peptides adhere to glass more than plastic
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What are leachables?
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Chemicals that migrate from the packaging into a formulated drug during normal use/storage
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Disadvantages of plastic packaging over glass packaging?
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Not as transparent, can soften/melt with heat
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Advantages of prefilled syringes?
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Reduces needle-stick injuries, less wastage with overfilling/measuring
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What are microneedles?
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Tiny needles, can only be used in intradermal delivery
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Disadvantages of needle-free delivery?
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Can cause pain/bruising/bleeding, bioequivalence harder, higher costs
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