Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmaceutics II > Exam 2 > Flashcards

Exam 2 Flashcards

1
Q
  • physiochemical properties of the drug and drug delivery system (drug release pattern - immediate/modified release, solubility, dissolution rate, permeability)
  • biological factors (physiological fluctuations along the GIT like pH/secretions/motility/emptying rate/residence time, biochemical variance, anatomical differences like surface area/thickness/blood supply), effects of food and other drugs
A

factors influencing oral bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

ratio of the concentrations of a drug in a mixture of two immiscible liquids at equilibrium (octanol/water), measure of lipophilicity, logD

A

distribution coefficient

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Biopharmaceutics Classifications of Drugs class with high solubility and high permeability

A

Class I

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Biopharmaceutics Classifications of Drugs class with low solubility and high permeability

A

Class II

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Biopharmaceutics Classifications of Drugs class with high solubility and low permeability

A

Class III

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Biopharmaceutics Classifications of Drugs class with low solubility and low permeability

A

Class IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

for oral drug delivery according to USP a drug substance is classified as highly ________ if the highest single therapeutic dose is completely _______ in 250mL or less (8 oz or less), should be studied over the pH range of 1.2 to 6.8 at 37 degrees C for stomach and small intestine

A

soluble

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

high _______ can be concluded when the absolute bioavailability is greater than or equal to 85%, considering the drug is chemically stable in the GIT

A

permeability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q
  • reducing particle size, do this to increase the surface area, enhance solubility, and improve bioavailability for Class II or IV drugs
  • example: Yonsa (abiraterone acetate), antiandrogen used for treatment of prostate cancer
  • example: Griseofulvin
  • example: Glyburide oral tablets, sulfonylurea, antidiabetic agent, administer with meals at same time each day, reduce hypoglycemia risk, absorption not affected by food
A

micronized formulations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

______ absorption is often irregular and unpredictable due to poor solubility and permeability, degradation by acid and enzymes, presystemic metabolism, variability in GI motility, effects of food

A

oral

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

medications that irritate the ___________ mucosa: antibiotics (doxycycline), NSAIDs, bisphosphonates, chemotherapeutic agents, KCl tablets, etc., pill size and texture (large pills, poorly formulated products)

A

esophageal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

take medications with full glass of water, remain upright for 30 minutes after taking, avoid laying down immediately after taking pills, make sure to swallow pills correctly without crushing or chewing them, for patients with difficulty swallowing pills discuss alternatives like liquid formulations or smaller pills

A

patient counseling on preventing pill-induced esophagitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

cephalic phase (20% of total acid secretion), gastric phase (pylorus only allows passage of liquid and small particles less than 2mm)

A

digestive (fed) phase of gastric emptying

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

not eating phase, migrating motor complex

A

interdigestive (fasted) phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q
  • phase I: 45-60 mins, no activity, rare contractions
  • phase II: about 30 mins, intermittent contraction, increasing intensity
  • phase III: 5-15 mins, intense and regular contractions, pylorus remains open, housekeeper waves
  • phase IV: short period of transition to phase I
  • all can transition to fed state with presence of food
A

migrating motor complex (MMC)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

________ release should not be taken before meals

A

delayed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

large surface area, mucosal folds, villi, microvilli, high blood flow which improves drug dissolution and absorption

A

small intestine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

varies with health, age, diet, concurrent drugs, fast transit means lower absorption, drugs that decrease GI motility may increase drug absorption

A

GI transit time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

much lower surface area compared to counterpart, not a major site of drug absorption, highly efficient reabsorption of water, rich in bacteria and bacterial enzymes (used for colon targeting)

A

large intestine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

absorption pathway, pores, solvent shift (moving fluids between cells)

A

convective transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

absorption pathway, carrier-mediated, needs energy, iron supplements, levothyroxine tablets, methotrexate

A

active transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

absorption pathway, diffusion supported by carriers, LATs, OCTs, OATs, PEPT1), carriers get saturated or inhibited, some vitamins, levodopa, metformin, trimethoprim, morphine, cimetidine, ranitidine, valacyclovir, fexofenadine, statins, beta-lactams, ACE inhibitors

A

facilitated transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

absorption pathway, vesicles, vesicular transport

A

transcytosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

absorption pathway, between cells, limited by tight junctions

A

paracellular permeation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

absorption pathway, actively transported out of cells through P-glycoproteins

A

efflux transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

absorption pathway, absorption of drugs along with fats, highly lipophilic drugs absorbed this way

A

transcellular diffusion and incorporation into lipid particles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

aqueous boundary layer (solubility and diffusion), epithelium (mucin, lipid bilayer), efflux transporters, chemical degradation, presystemic and first pass metabolism

A

barriers in GI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

drug metabolism by GIT and hepatic enzymes, decreased bioavailability

A

presystemic metabolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

recirculation of drug, some drugs undergo this, biliary excretion of the drug and intestinal reabsorption, hepatic conjugation and intestinal deconjugation, rifampin is an example of a drug that does this

A

enterohepatic circulation (EHC)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

alter gastric emptying time, alter pH, formation of drug-food components complex, increase viscosity of GI content, stimulate GI secretions, competes for specialized absorption mechanism, food-induced changes in pre-systemic metabolism and blood flow, food as a dissolution medium and absorption promoter

A

effects of food on oral drug delivery systems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

delay the onset of therapeutic activity, avoid or reduce acute toxicity by keeping Cmax lower (tamsulosin, if taken with food can decrease adverse effects, safer)

A

delayed or slower absorption rate because of food

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

instability of drug in gastric fluid, chelation (complex interaction) with ions in the food, adsorption of the drug to food components, increased first-pass metabolism, leads to less drug available to have clinical effect

A

decreased absorption because of food

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

longer time for dissolution in the stomach, increased solubilization of the drug (pH effect), absorption with fats, reduced first pass metabolism

A

increased absorption because of food

34
Q

viscous material empties at a slower rate in comparison to less viscous for increased gastric emptying time, delayed onset, decreased rate, prolong contact/stay in the gastric environment may affect drug stability, may improve bioavailability for drugs that dissolve slowly in the stomach at lower pH

A

food increases the viscosity of GI content

35
Q

drug food interactions forming an insoluble complex, drug chelation, prevents drug absorption, dietary supplements

A

complexation

36
Q

surface property, not chemical interaction, macromolecule complex (poor or no absorption), dietary fiber (cellulose, chitosan, pectin, xanthan gum, sodium alginate)

A

adsorption

37
Q

food containing lipids stimulates secretion of bile, bile emulsifies and solubilizes lipids, influence drug absorption of lipophilic drugs

A

stimulation of GI secretions

38
Q

improved absorption of lipophilic drugs (may be absorbed from small intestines along with digested fats), reduced first pass metabolism (if through lymphatic route - the lymphatic system does not connect to the portal circulation)

A

competition between food components and drugs for specialized absorption mechanisms

39
Q

food components may inhibit CYP3A4 in intestinal cells leading to increased bioavailability of CYP3A4 substrates (stains, benzodiazepines, immunosuppressants), grapefruit inhibits drug metabolism by interfering with hepatic and intestinal CYP450 (atorvastatin and grapefruit leads to higher plasma concentration of atorvastatin)

A

food-induced changes in pre-systemic metabolism

40
Q

monoamine oxidase metabolizes tyramine, if tyramine consumed while taking MAO inhibitor the tyramine levels will increase (phenelzine, selegiline), tyramine increases NE levels leading to hypertensive crisis, food high in tyramine (aged cheeses, cured meats, fermented foods, certain types of fermented/pickled foods, beans, alcoholic beverages)

A

tyramine-containing foods/beverages

41
Q

food _________(increases/decreases) blood flow rate and increases bioavailability of compounds, hepatic blood flow, oral bioavailability

A

increases

42
Q

increased solubilization of drug in food components, fatty food improves the dissolution of lipophilic drugs, use lipid based drug delivery systems (add a lipid as an excipient), food slows gastric emptying rate and that may improve dissolution rate

A

food promotes dissolution and absorption

43
Q

dorsal tongue, gingiva, hard palate are keratinized (strong and hard) or nonkeratinized?

A

keratinized

44
Q

cheeks, inner lips, ventral tongue, floor of mouth, soft palate are keratinized or nonkeratinized?

A

nonkeratinized

45
Q

where is drug absorption faster (keratinized or non)?

A

nonkeratinized

46
Q
  • complex mixture of secretions from salivary glands, oral, pharyngeal, nasal mucosa, mostly water but also has electrolytes, buffers, mucins, digestive enzymes, statherins (remineralization), histatins (antimicrobial/antifungal)
  • helps with transmucosal drug release (water-rich fluid), dilution and buffering, mucoadhesive dosage forms, excessive saliva flow (salivary washout of dosage form), digestive enzymes (stability of some drugs may be affected)
A

saliva

47
Q

applied to oral mucosa (mucus membrane), rapid absorption, fast onset of action (highly vascular mucosal lining, suitable for emergency like nitroglycerin), no need for water, bioadhesive/mucoadhesive (buccal forms can provide ER), avoid the first pass metabolism (increase bioavailability and reduce adverse effects, reach required concentration with lower dose which decreases adverse effects), suitable for patients with dysphagia, unconscious or incapacitated, nauseated, patients on reduced liquid intake

A

oral transmucosal drug delivery

48
Q

high doses cannot be administered because small surface area of absorption and limited residence time (unless bioadhesive), not suitable for bitter or irritating drugs or excipients that stimulate saliva production and promote swallowing, not suitable for uncooperative patients, patients may be restricted from eating, drinking, smoking, some dosage forms may affect oral hygiene, dentures, braces, damaged mucosa, precautions with products containing aspartame in patients with PKU

A

disadvantages of oral transmucosal drug delivery

49
Q

administered under the tongue (small and flat tablet, compressed lightly), thin mucosa and highly vascular (fast absorption and increased AUC because avoids first pass metabolism), suitable for angina (nitroglycerin), pain (sufentanil, buprenorphine), migraine (ergotamine), schizophrenia (asenapine)

A

sublingual tablets

50
Q

small flat tablet or film intended for oral transmucosal drug delivery, administered in the cheek or applied to upper gum, absorption is slower compared to sublingual (thicker mucosa and less permeable), Belbuca (buprenorphine), Sitavig (acyclovir), Oravig (miconazole)

A

buccal tablet/film

51
Q

maximize the contact of the patch/tablets with oral mucosa to improve absorption, retain the dosage form in the oral cavity (patient can talk, drink, eat), bioadhesive polymers or buccal patch bind to gingival mucosa

A

mucoadhesive/bioadhesive

52
Q

held in the mouth and allowed to dissolve slowly, local effect on the mouth and throat (clotrimazole) or systemic effect (fentanyl), tell patients how to take medication/storage and disposal/how to keep away from young children

A

lozenge/troche

53
Q

creates a mist of liquid particles, metered valve releases contents in a controlled and uniform dose, Nitrolingual (nitroglycerin) translingual solution, can have local effects for cosmetics or dry mouth

A

aerosol solution/spray

54
Q

nicotine (smoking cessation aid, OTC, bound to an ion exchange resin), chewing releases drug (chew slowly and stop chewing occasionally, most of the drug released from the gum is absorbed by oral cavity, fast onset of action and avoids first pass metabolism

A

medicated chewing gum

55
Q

unique dosage form for persistent hemorrhoids, designed to get drug to site of action, hold drug at site of action for extended period (slit for flatulence), available only as compounded product, does not get lost in rectum but remains at point of application/insertion, treats internal and external hemorrhoids at same time

A

rectal rockets

56
Q

highly vascular, superior rectal vein is portal (first pass metabolism), middle and inferior rectal veins drain into the inferior vena cava (avoid first pass metabolism), may result in erratic drug absorption (variable)

A

rectal vasculature

57
Q

minimize the effect of first pass metabolism, avoid problems of oral drug administration like GI irritation, inactivation of drug, effect of food, suitable for patients unable to swallow (dysphagia, nausea vomiting, unconscious, infants/young children), provide local action (IBD, hemorrhoids, constipation)

A

advantages of rectal drug delivery

58
Q

poor patient acceptance, erratic drug absorption from rectal route due to poor technique of insertion or disease conditions like diarrhea, not suitable for large volumes or drugs that irritate the rectum (unless laxative because large volume or irritation induce bowel movement)

A

disadvantages of rectal drug delivery

59
Q

what type of suppository base melts at body temperature to release the drug (fatty or water soluble)?

A

fatty

60
Q

what type of suppository base dissolves to release the drug (fatty or water soluble)?

A

water soluble

61
Q

either melts or dissolves in rectal fluid, should be solid at room temperature for ease of insertion, non-irritating to rectal mucosa (water soluble bases are hygroscopic and irritant), should provide suitable drug release profile

A

desirable properties of suppository bases

62
Q

solution or suspension, administered/injected into the rectum for cleansing/evacuating/local drug effect, Rowasa (mesalamine)

A

rectal enema

63
Q

Cortifoam (hydrocortisone) and Uceris (budesonide) are examples of this, spreads well into the rectum, provides uniform coverage, retains in the rectum better, used for treatment of ulcerative colitis of the rectum (ulcerative proctitis)

A

rectal foam

64
Q

diazepam comes in this form, for status epilepticus and breakthrough seizures, easy to administer in emergency, rapid onset of action

A

rectal gel

65
Q

Rectiv (nitroglycerin) is an example of this

A

rectal ointment

66
Q

hydrocortisone comes in this form, reduces inflammation, treats itching or swelling caused by hemorrhoids or idiopathic external anal pruritis, may require applicator or syringe

A

rectal cream

67
Q

protective mucus, complex mixture of proteins and polysaccharides, suitable for transmucosal drug delivery, pH of this varies by age (lower at reproductive age)

A

vaginal fluid

68
Q

good surface area and rich blood supply (avoids first pass metabolism and problems related to GIT), permeable to a wide range of compounds (peptides, proteins, steroids), provides targeted drug delivery to the uterus and surrounding tissues, poor patient compliance (difficult to use, poor patient acceptance, interfere with sexual activity, lack of retention), variability in drug absorption due to age, menstrual cycle, menopause, pregnancy

A

vaginal drug delivery

69
Q

Cleocin (clindamycin) ovules, miconazole suppositories, terconazole suppositories all examples of this, oleaginous base

A

vaginal suppositories (ovules)

70
Q

ointment, cream, gel, foam, uniform coverage and ease of spreading, easy to adjust dose, suitable for individualized medicine

A

vaginal semisolid dosage forms

71
Q

1 day treatment, administer one applicatorful intravaginally at bedtime

A

Monistat vaginal ointment

72
Q

medications to treat vulvovaginal candidiasis, bacterial vaginosis, and vulvar and vaginal atrophy associated with menopause come in this form

A

vaginal cream

73
Q

medications to treat bacterial vaginosis, secondary amenorrhea, spermicide contraceptive, cervical ripening come in this form

A

vaginal gel

74
Q

requires an applicator, provides uniform distribution over a large surface area, VCF (insert one applicatorful no more than one hour prior to intercourse - effective for up to one hour)

A

vaginal foam

75
Q

NPO, elegant, no leak out, disintegrate or dissolve in vaginal fluid, could be bioadhesive, ease of application using an applicator, Vagifem/Yuvafem (estradiol)

A

vaginal tablets

76
Q

softgel capsule (Imvexxy), suppository (Intrarosa), oblong shaped tablet (Endometrin), extended release device (Cervidil)

A

vaginal insert

77
Q

solid dosage forms that dissolve when in contact with vaginal fluids, ease of application and longer retention time, more acceptable as compared with vaginal cream or gel, VCF

A

vaginal film

78
Q

circular drug delivery system, made of flexible and non-irritating polymers, provides controlled/sustained drug release, Estring, Femring, Annovera, NuvaRing, EluRyng, EnilloRing, Haloette

A

vaginal ring

79
Q

kills sperm cells, blocks cervix opening, absorbs and traps the sperm, Today (nonoxynol-9)

A

vaginal sponge

80
Q

administer medications directly into urethra, localized treatment of conditions affecting the urinary tract (antibacterial, erectile dysfunction, urinary incontinence, urinary infections, cancer)

A

urethral drug delivery

Pharmaceutics II (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions