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54 CNS > Pharmaceutical Technology 2 > Flashcards

Pharmaceutical Technology 2 Flashcards

1
Q

Types of injections

A
  1. Intramuscular - into muscle
  2. Subcutaneous - into subcutaneous layer
  3. Intravenous - into vein
  4. Intradermal - into epidermis
  5. Intrathecal - into spinal cord
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2
Q

(Intrathecal injections) Drug delivered into ______ flows directly to the ____.

A

CSF
Brain

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3
Q

How can drugs be administered for intrathecal injections?

A

a. Into reservoir (Ommaya)
b. Via lower back

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4
Q

CSF is a clear solution made up of?

A

99% water
1% protein, ions, neurotransmitters & glucose

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5
Q

pH of CSF

A

~7.3

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6
Q

Volume of CSF

A

150mL, 430-530mL produced per day

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7
Q

CSF has variable ____, ____ and ___.

A

Viscosity
Flow rate
Pressure

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8
Q

Can intrathecal cross the BBB?

A

Yes

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9
Q

Advantages of parenteral delivery 1

A

Bypasses hepatic 1st pass metabolism

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10
Q

Advantages of parenteral delivery 2

A

Can control dosage
- Relatively low drug concentration and low toxicity

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11
Q

Advantages of parenteral delivery 3

A

Direct access to brain (intrathecal)

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12
Q

Advantages of parenteral delivery 4

A

Sustained release (intramuscular depot, intrathecal reservoirs)

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13
Q

Advantages of parenteral delivery 5

A

Ideal for non-compliant, unconscious or dysphagic patients

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14
Q

From blood to brain, drug solution flows through ______.

A

Circulatory system
- Reticuloendothelial system (RES)
- Unless there is active targeting, drug will distribute everywhere

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15
Q

Drugs must bypass ____ to access the brain.

A

BBB

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16
Q

The blood brain barrier blocks uptake of __% of small molecular drug candidates.

A

98%

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17
Q

Types of transportation across BBB

A

Paracellular (tight junctions)
Transcellular

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18
Q

Examples of active efflux transporters

A

P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multi-drug resistance proteins (MRP)

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19
Q

What are active efflux transporters?

A

Removes drugs from organ (brain) into the lumen (blood)

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20
Q

Types of transporters in BBB

A
  1. Active efflux
  2. Carrier mediated (CMT)
  3. Receptor-mediated (RMT)
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21
Q

Modified Lipinski’s for CNS - MW

A

<450 Da

22
Q

Modified Lipinski’s for CNS - hydrogen bond donors

A

<3

23
Q

Modified Lipinski’s for CNS - hydrogen bond acceptors

A

<7

24
Q

Modified Lipinski’s for CNS m- LogP

A

1-3

25
Q

Modified Lipinski’s for CNS - ionisation state

A

Unionised

26
Q

Delivery system - solutions

A

a. drug molecules
b. proteins/peptides

27
Q

Delivery system - suspensions

A

a. Nano/microemulsions
b. Liposomes and other lipid-based self-assembled structures
c. Nanoparticles

28
Q

Common excipients of solutions for injection

A
  1. Diluents
  2. Buffer salts
  3. Tonicity adjusters
  4. Preservatives (minimal for intrathecal)
  5. Stabilisers/co-solvent
29
Q

pH consideration for parenteral delivery

A

Ideally 7.4 but wide range tolerated
Intramuscular: 3-11
Subcutaneous: 3-6

30
Q

Tonicity consideration for parenteral delivery

A

280-290 mOsm/L for large volume parenteral
Hypertonic > hypotonic (can increase with tonicity adjuster)

31
Q

Particle size consideration for parenteral delivery

A

No visible particles (more for IV than SC/IM)

32
Q

Benzyl alcohol

A

Preservative

33
Q

Ethanol

A

Solvent

34
Q

Glycine

A

Solvent

35
Q

PEG (mixed)

A

Solvent

36
Q

Propylene glycol

A

Solvent

37
Q

Glycerin/glycerol

A

Solvent/tonicity adjustment

38
Q

Glycine

A

Solvent/tonicity adjustment

39
Q

Thiomersal

A

Preservative

40
Q

Mannitol

A

Tonicity adjusting agent / cryoprotectant

41
Q

Sodium acetate, citrate, and phosphates (mixed), lactate

A

Buffer

42
Q

Function of reservoir in infusions

A

Refilling

43
Q

Function of catheter in infusions

A

Delivery

44
Q

Function of pump in infusions

A

Automate dosing

45
Q

Biocompatible material in infusion

A

Titanium

46
Q

Haloperidol formulation

A

50mg/mL or 100mg/Ml injection

47
Q

Site of administration of Haloperidol

A

IM into gluteal region

48
Q

Interval between doses for Haloperidol

A

4 weeks

49
Q

Half-life of Haloperidol

A

3 weeks

50
Q

Baclofen route od adminitration

A

Intrathecal injection

51
Q

Baclofen concentration in ____ is 100x higher than after _________.

A

CSF
Oral administration

54 CNS (13 decks)

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