UNIT 2 (BIOPHARMACEUTICALSㅡFATE OF DRUG) Flashcards

1
Q

• the study of the physicochemical properties of the drug and the drug product, in vitro, on the bioavailability of the drug, in vivo, to produce a desired therapeutic effect.

A

BIOPHARMCEUTICS

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2
Q
  • It is the study of the kinetics of absorption, distribution, metabolism, and excretion (ADME) of drugs and their corresponding pharmacologic, therapeutic, or toxic effects in animals and man.
A

PHARMACOKINETICS

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3
Q

• The absorption process is driven by the concentration gradient across the membrane, with the passage of drug molecules occurring primarily from the side of high concentration.

Described by _____________

A

• Fick’s first law of Diffusion

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4
Q

• involves the aqueous channels or pores through which hydrophilic drugs can pass.

○ Occurs in the jejunum and proximal tubules of kidneys

○ Absent in the stomach and the lining of the urinary bladder

A

Filtration

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5
Q

• Drugs are better absorbed in __________ form.

A

unionized

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6
Q

• This type of transport is thought to involve membrane components that may be enzymes or some other type of agent capable of forming a complex with the drug (or other agent) at the surface membrane.

A

SPECIALIZED TRANSPORT MECHANISM

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7
Q

• Under normal circumstances, a drug may be expected to remain in the stomach for 2 to 4 hours (_________________) and in the small intestine for 4 to 10 hours

• The gastric emptying time for a drug is most rapid with a fasting stomach, becoming slower as the food content is increased.

A

gastric emptying time

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8
Q

• ↑ increase GET

A

▪ High fat /fatty foods

▪ Cold food

▪ Gastric ulcers

▪ Stress

▪ Vigorous exercise

▪ Lying on the left side

▪ Drugs (Antidiarrheal

/antimotility agents)

▪ Hunger

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9
Q

• ↓ decrease GET

A

▪ Spicy foods

▪ Extreme temp. of meal

▪ Gastrectomy

▪ Depression

▪ Mild Exercise

▪ Lying on right side

▪ Motility enhancing agents:

(metoclopramide, domperidone, cisapride)

▪ Diabetes Mellitus

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10
Q
  • They form a subtype of solid solvates in which water molecules are incorporated into the crystal lattice of a compound

o The possibility of solid APIs to exist at different levels of hydration represents another way to improve the APIs’ properties by altering their solid state structures.

A

● Hydrates

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11
Q

● The drug–protein complex-

● reversible,

● involves albumin (globulins also participate in the binding of drugs, particularly some of the hormones)

● Entails formation of relatively weak bonds (van del Waals, hydrogen, ionic)

● Binding capacity is saturable

A

Protein-binding

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12
Q

o NOT exposed to the body’s detoxification (metabolism) processes

o NOT filtered through the renal glomeruli

A

BOUND DRUG

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13
Q

o Serves as a reservoir or depot (only released when the level of free drug in the blood is no longer adequate to ensure protein saturation)

A

INACTIVE PORTION

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14
Q

● the major process by which foreign substances, including drugs, are eliminated from the body

● Biotransformation indicates the chemical changes to drugs within the body as they are metabolized and altered by various biochemical mechanisms.

A

Metabolism

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15
Q

▪ an inactive parent compound, may be converted to an active therapeutic agent by chemical transformation in the body.

A

Prodrugs

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16
Q

● refers to both metabolism and excretion

● The kidney is the most important organ for excreting drugs and their metabolites.

A

Elimination

17
Q

The rate of reabsorption is _____________ to the concentration of drug in un-ionized form.

A

proportional

18
Q
  • Refers to the comparison of bioavailabilities of different formulations, drug products, or batches of the same drug products
A

Bioequivalence

19
Q

• Describes the rate and extent to which an active drug ingredient or therapeutic moiety is absorbed from a drug product and becomes available at the site of action

A

Bioavailability

20
Q

Bioavailability data

A

the amount or proportion of drug absorbed from a formulation or dosage form

the rate at which the drug was absorbed

the duration of the drug’s presence in the biologic fluid or tissue correlated with the patient’s response

the relationship between drug blood levels and clinical efficacy and toxicity.

21
Q

• According to the FDA (5), the in vivo bioavailability of a drug product may be determined by:

A

o measurements of the concentration of the active drug ingredient

o its therapeutic moiety

o its metabolite(s) in the blood or urine

pharmacological effects

22
Q
  • contain the same therapeutic moiety but are different salts, esters, or complexes of that moiety
  • different dosage forms or strengths
  • Different dosage forms and strengths within a product line by a single manufacturer
  • extended-release products when compared with immediate- or standard-release formulations of the same active ingredient
  • Ex. Tetracycline hydrochloride vs tetracycline phosphate complex)
  • Ex. Quinidine sulfate tablets vs Quinidine sulfate capsules
A

Pharmaceutical Alternatives

23
Q
  • are pharmaceutical equivalents or pharmaceutical alternatives whose rate and extent of absorption do not show a significant difference when administered at the same molar dose of the therapeutic moiety under similar experimental conditions, either single dose or multiple dose.

Some PE and PA may be equivalent in the extent of their absorption but not in their rate of absorption and yet may be considered bioequivalent because such differences in the rate of absorption are intentional and are reflected in the labeling, are not essential to the attainment of effective body drug concentrations on chronic us

A

Bioequivalent Drug Products

24
Q
  • have the SAME pharmacokinetic and pharmacodynamic properties.
  • have been proven bioequivalent and the FDA believes they can be expected to have the same clinical effect and adverse-events profile.
  • generally, are considered most appropriate for substitution.
A

Therapeuic Equivalents

25
Q

• are achieved by direct application of the drug to the desired site of action, such as the eye, nose, or skin.

A

Local effects

26
Q

• result from the entrance of the drug into the circulatory system and transport to the cellular site of its action.

A

Systemic effects

27
Q

● Drugs are most frequently taken by oral administration

● Most are taken for the systemic drug effects

● ADVANTAGE

o Most natural

o Uncomplicated

o Convenient

o Safe

● DISADVANTAGE

o slow drug response (compared with parenterals)

o chance of irregular absorption of drugs (type of food in GI)

o Destruction of certain drugs by the acid reaction of the stomach or by gastrointestinal enzymes

A

ORAL ROUTE

28
Q

● Some drugs are administered rectally for their local effects and others for their systemic effects.

● The rectum and the colon can absorb many soluble drugs

● Rectal administration for systemic action may be preferred for drugs destroyed or inactivated by the environments of the stomach and intestines.

● may also be indicated when the oral route is precluded because of vomiting or when the patient is unconscious or incapable of swallowing drugs safely without choking

A

RECTAL ROUTE

29
Q

● parenteral is derived from the Greek words—

o para : meaning beside

o Enteron : meaning intestine

● which together indicate something done outside of the intestine and not by way of the alimentary tract

A

PARENTERAL ROUTE

30
Q

Three primary routes

A

o Subcutaneous

o Intramuscular

o Intravenous

31
Q

OTHER ROUTES

A

● Ocular

● Otic

● Nasal

● Lungs

● Vagina

● Urethra