Block I - Kinetics - A-D Flashcards

1
Q

Site of absorption: oral

A

Mouth -> stomach/SI; safe, economic, convenient; acidic best in stomach; basic best in SI

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2
Q

Site of absorption: sublingual

A

Under tongue -> cap network -> systemic circ; Diffuse rapidly, bypass GI environ

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3
Q

Site of absorption: IM

A

Aqeous: rapid; Depot: delayed release.

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4
Q

Site of absorption: IV

A

Rapid plasma concentration release. 100% bioavailable. Cannot be recalled.

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5
Q

Site of absorption: inhaled

A

Goes to brain quickly. Pt may have hard time controlling dose.

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6
Q

Site of absorption: transdermal

A

Lipophilic drugs absorbed best this way. Slow/sustained delivery. Rate of absorption can vary (based on underlying tissue composition). Bypasses liver first-pass.

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7
Q

Site of absorption: parenteral

A

Bypass enteric system (eg IV, IM subcut). Used to treat unconscious pt, when quick delivery is needed, drugs unstable in GI. High bioavailability; cannot be recalled.

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8
Q

Site of absorption: epidural

A

Administered via catheter (slow admin). Bypasses blood-brain barrier. Used for pain relief.

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9
Q

Site of absorption: intrathecal

A

Injected directly into subarachnoid space. Used when rapid CNS effects needed. One injection in contrast with epidural (continuous).

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10
Q

Site of absorption: rectal

A

Some of drug bypasses liver first pass. Ideal for comatose/vomiting pts. May be incomplete/erratic absorption.

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11
Q

Method for delaying absorption: delayed released preparations

A

Oral meds with special coating to extend time over which drug is released. Good for drugs with short half life.

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12
Q

Method for delaying absorption: depot preparations

A

IM injections with suspension of drug in non-aqueous solution. Slowly dissolves, sustained-release.

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13
Q

Method for delaying absorption: implanted pumps

A

Release drugs subQ; via pump (insulin) or solid (hormones).

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14
Q

Method for delaying absorption: transdermal patches

A

Sustained release of drug to achieve systemic effects. Absorption depends of location and lipid solubility of drug.

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15
Q

Method for delaying absorption: pH sustained preparations

A

Drugs manufactured to withstand very low pH in order to control rate of absorption to stay within therapeutic window

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16
Q

Method for delaying absorption: patient controlled administration (PCA)

A

Pts self-administer medication at a predetermined dose.

17
Q

Bioavailability

A

Fraction of administered drug that reaches systemic circulation. Compare to plasma levels of drug when given IV.

18
Q

Factors influencing bioavailability: 1st pass hepatic metabolism

A

Drug rapidly metabolized in liver during first pass, amt of drug to gain systemic circ access decreased.

19
Q

Factors influencing bioavailability: solubility of drug

A

Very hydrophilic drugs poorly absorbed b/c can’t cross cell membrane. Very hydrophobic drugs poorly absorbed b/c can’t gain access to cell surface. Optimal: drug that is mostly hydrophobic but still some solubility in aqueous solutions.

20
Q

Factors influencing bioavailability: chemical instability

A

Some drugs unstable in gastric pH.

21
Q

Factors influencing bioavailability: nature of drug formulation

A

Factors that influence ease of dissolution and thus alter absorption; particle size, salt form, enteric coatings, etc.

22
Q

Difference between plasma conc curve: IV/IM/oral

A

IV: high peak, IM: med peak, oral: low peak

23
Q

Loading dose

A

Single dose of drug given to elevate plasma levels to steady state.

24
Q

Changes in stomach pH and affect on absorption of acidic and basic drugs

A

Acidic drugs: like to be absorbed in stomach (pH 1-2). If pH lowered in stomach, acidic drugs like. If raised (with meal) then it don’t like. Basic drugs: like to be absorbed in SI (pH 3-6). If pH raised in stomach, may be absorbed there.

25
Q

Proteins drugs bind

A

Albumin (acidic strong, basic weak), alpha 1 glycoprotein, tracer proteins; free drug (active)

26
Q

How blood-brain barrier prevents drugs from entering brain

A

Tightly packed endothelial cells of capillaries require drugs to be small, nonpolar, and lipophilic to go thru active transporters from blood across BBB.

27
Q

Volume of distribution

A

Volume of fluid that total amount of drug would have to occupy to have same concentration as blood plasma.

28
Q

Physiologic volume vs volume of distribution

A

Physiologic volume = extracellular + intracellular fluid. If drug bound to tissue, then volume of distribution can be well over amount of plasma or total body water.

29
Q

Small VoD

A

Stays in circulatory system. More acidic drugs, low lipid solubility, high plasma protein binding, low tissue binding.

30
Q

Large VoD

A

Hightly tissue bound. Basic drugs (greater tissue binding than acidic), high lipid solubility, low plasma protein binding, high tissue binding.