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PY366 Depression, anxiety and schizophrenia > Long acting parenteral solutions > Flashcards

Long acting parenteral solutions Flashcards

1
Q

what are long acting parenteral formulations

A
  1. long acting injections
    - oily solutions
    - oily suspensions
    - aqueous suspensions
    - microspheres
    - liposomes
  2. implants
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2
Q

why are long acting injectables used

A
  1. improved safety and efficacy
  2. improved patient compliance and outcomes
  3. cost reduction
  4. life cycle optimisation
  5. allows bolus delivery for some drugs that otherwise could require slow IV administration
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3
Q

what are the idealised characteristics of long acting injections

A
  1. controlled delivery over 1 week to 6 months from single injection
  2. biodegradable/biocompatible carrier materials
  3. easy to manufacture, store and administer product
  4. compatible with sensitive molecules
  5. compatible with conventional drugs
  6. low or high loading capability
  7. can deliver water soluble or water insoluble products
  8. provide proprietary protection
  9. low toxicity
  10. all generally recognised as safe excipients
  11. do not require drug modification
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4
Q

what are the benefits of long acting products and what are they used for

A
  1. treatment of resistant patients
  2. delivery of antipsychotics
  3. improving convenience of chronic care products
  4. improvement in safety profiles
  5. insulins
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5
Q

what are the types of sustained release dosage forms

A
  1. aqueous suspension injections
  2. oily injections
  3. implants
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6
Q

describe the use of a long acting antipsychotic injection

A
  1. deep IM injection which forms a depot
  2. drug released at fairly steady rate into blood, typically over several weeks
  3. 30% of patients with schizophrenia are treated with prolonged release injectable antipsychotic in UK
  4. may overcome poor adherence to oral antipsychotic regimens and help improve relapse rate
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7
Q

what are the disadvantages of long acting injections

A
  1. IM injection is uncomfortable and may produce injection site reactions
  2. dose titration may be more difficult than with immediate acting oral formulations
  3. adverse effects may persist until drug has been cleared from its depot site
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8
Q

name some antipsychotic LAI preparations

A
  • haloperidol decanoate (FGA)
  • olanzapine embonate
  • both are every 2-4 weeks
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9
Q

what are the advantages of depot and other long acting antipsychotic injections from a healthcare professional perspective

A
  1. reduced necessity for tablets or capsules to be taken on daily basis
  2. reduced uncertainty about amount of medicine taken or not taken
  3. no influence of first pass metabolism so improved bioavailability
  4. more consistent delivery of antipsychotic with more stable plasma levels over time
    - minimising side effects and variations in symptom control
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10
Q

what are the disadvantages of depot and other long acting antipsychotic injections from a healthcare professional perspective

A
  1. pain, erythema, swelling at injection site as well as nodule formation
  2. risk of damage to nerves, arteries or veins
  3. if side effects occur, they will be prolonged until plasma level falls
    4.can take several weeks of plasma levels to reach steady state
  4. the need to confirm efficacy and tolerability to the oral formulations of the non oil based LAI where required
  5. injection technique competence, assessment and training required
  6. dislike or phobia of needles
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11
Q

give examples of advantages of depot and other long acting antipsychotic injections from a patient perspective

A
  1. don’t have to remember to take medicine everyday
  2. may have fewer side effects with an injection as levels in blood don’t rise and fall as much
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12
Q

give examples of disadvantages of depot and other long acting antipsychotic injections from a patient perspective

A
  1. dislike of needles
  2. if you do develop side effects, they may persist for several weeks after injection is stopped
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13
Q

what are the different mechanisms used to give long action

A
  1. prodrug dissolved in oil
  2. polymeric microspheres
  3. poorly water soluble salt suspended in water
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14
Q

describe how ester groups are used for depot injectables (LAI)

A
  1. saturated fatty acid
  2. used to form prodrugs
  3. increases lipophilicity of drug
  4. used to decrease aqueous solubility of drugs
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15
Q

describe the properties of the risperidone long acting injection

A
  1. micrometer sized biodegradable poly microspheres which are loaded with risperidone and suspended in sterile saline
  2. diluent contains carmellose sodium, anhydrous citric acid, polysorbate 20 and sodium hydroxide
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16
Q

what is paliperidone palmitate

A
  1. ester prodrug of paliperidone
  2. aqueous suspension of particles and nanocrystal
17
Q

what are the properties of pamoic acid

A
  • also called embolic acid
  • poorly water soluble salt
  • decreases the water solubility of olanzapine
18
Q

what is olanzapine embonate

A
  1. salt of embolic acid and olanzapine suspended in aqueous solution
  2. injected into gluteal muscle
  3. 2 components of the salt slowly dissociate into separate molecular compounds- olanzapine and embolic acid
  4. rate of dissolution of salt is slow, allowing for gradual release of olanzapine into circulation over 2-4 weeks
19
Q

what are the potential challenges for long acting formulations

A
  1. creating zero order kinetics
  2. chemical modifications of parent drug
    - creates new API with attendant requirements to support approval for marketing
  3. use of non GRAS excipients
    - requires demonstration of safety of new materials
  4. consistent quality of polymeric materials
  5. poor drug stability
  6. burst effect and dose dumping
20
Q

what are implants

A
  1. sterile, solid drug products made by compression, melting or sintering
    - eg. goserelin acetate implant (zoladex)
21
Q

what is the carmustine matrix implant

A
  1. polifeprosan 20
    - biodegradable polyanhydride copolymer
  2. carmustine- released as copolymer degrades
    - 70% degrades in 3 weeks
22
Q

what is the goserelin matrix implant

A
  1. SC into upper abdominal wall
  2. continuous release over 28 days
  3. goserelin dispersed in matrix
  4. matrix is copolymer of D, L lactic acid and glycolic acids

PY366 Depression, anxiety and schizophrenia (8 decks)

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