Top 200 Drug Podcasts - Set 6 - Metabolism And Elimination

Front 1

Hydrocodone/APAP

Back 1

Hydrocodone is metabolized by CYP 2D6 to an active metabolite (hydromorphone). APAP is predominantly metabolized via conjugation with either sulfate or glucuronide. Minor pathways include metabolism via CYP 1A2 & 2E1. Metabolites of both hydrocodone and APAP are excreted in the urine.

Front 2

Atorvastatin

Back 2

Metabolized by CYP 3A4.

Front 3

Levothyroxine

Back 3

Metabolized to T3. Both T4 & T3 are primarily eliminated via the kidneys.

Front 4

Lisinopril

Back 4

Excreted unchanged in urine.

Front 5

Amoxicillin

Back 5

Excreted unchanged in urine.

Front 6

Esomeprazole

Back 6

Metabolized by CYP 2C19 & 3A4.

Front 7

Clopidogrel

Back 7

Metabolized by CYP 2C19 & 3A4.

Front 8

Metoprolol Tartrate

Back 8

Metabolized by CYP 2D6.

Front 9

Montelukast

Back 9

Metabolized by CYP 2C9 & 3A4.

Front 10

Escitalopram

Back 10

Metabolized by multiple enzyme systems. Hence the inhibition of a single enzyme may not appreciably decrease clearance.

Front 11

Albuterol Inhaler

Back 11

Excreted renally either as the parent compound or the primary metabolite. SULTIA3 (sulfotransferase) is thought to be the primary enzyme responsible for albuterol metabolism.

Front 12

Simvastatin

Back 12

Simvastatin is a lactone prodrug. Hydrolysis of the lactone ring via carboxylesterases produces the active, beta-hydroxyacid form. Simvastatin undergoes extensive 1st pass metabolism via CYP3A4. The metabolites undergo biliary secretion, followed by excretion in the feces.

Front 13

Amlodipine

Back 13

Metabolized by the liver and excreted in the urine, predominantly as inactive metabolites.

Front 14

Azithromycin

Back 14

Excreted primarily in the bile as unchanged drug.

Front 15

Metformin

Back 15

Actively secreted in the urine, predominantly as unchanged drug.

Front 16

Metoprolol Succinate

Back 16

Metabolized by CYP 2D6.

Front 17

Hydrochlorothiazide

Back 17

Excreted in the urine as unchanged drug.

Front 18

Rosuvastatin

Back 18

Metabolized by CYP 2C9 and excreted mainly in the feces as unchanged drug.

Front 19

Furosemide

Back 19

Excreted in the urin and the feces.

Front 20

Warfarin

Back 20

Metabolized primarily by CYP 2C9, but is also metabolized via 2C8, 2C18, 1A2, and 3A4. Excreted in the urine.

Front 21

Fluticasone & Salmeterol

Back 21

Both are major substrates for CYP 3A4.

Front 22

Ibuprofen

Back 22

Oxidized in the liver, primarily by CYP 2C9. Excreted in the urine as metabolites.

Front 23

Sertraline

Back 23

Metabolized by multiple CYP enzymes and excreted in the urine and feces as metabolites.

Front 24

Valsartan

Back 24

Excreted primarily in the feces, and somewhat in the urine, as unchanged drug. [Approximately 9% is metabolized by CYP 2C9 to an inactive metabolite.]

Front 25

Zolpidem

Back 25

Metabolized mainly by CYP 3A4 and 2C9. Excreted in the urine and feces as inactive metabolites.

Front 26

Oxycodone/APAP

Back 26

Oxycodone is metabolized by CYP 3A4 & 2D6 to active metabolites. APAP is predominantly metabolized via conjugation with either sulfate or glucuronide. Metabolites of both are excreted in the urine.

Front 27

Duloxetine

Back 27

Metabolized in the liver by CYP1A2 and 2D6. Excreted in the urine (mainly) and feces, primarily as metabolites.

Front 28

Quetiapine

Back 28

Metabolized in the liver by CYP 3A4 to an active metabolite. Excreted in the urine (mainly) and feces, primarily as metabolites.

Front 29

Venlafaxine

Back 29

Metabolized in the liver by CYP 2D6. It has one active metabolite (O-desmethylvenlafaxine).

Front 30

Tamsulosin

Back 30

CYP 2D6 & 3A4

Front 31

Alprazolam

Back 31

Metabolized in the liver by CYP 3A4 and excreted in the urine. [It has two active metabolites.]

Front 32

Valsartan / Hydrochlorothiazide

Back 32

Valsartan is excreted primarily in the feces, and somewhat in the urine, as unchanged drug. [Approximately 9% is metabolized by CYP 2C9 to an inactive metabolite.] Hydrochlorothiazide is excreted in the urine as unchanged drug.

Front 33

Trazodone

Back 33

Metabolized by CYP 3A4 and does have an active metabolite.

Front 34

Pioglitazone

Back 34

Metabolized by CYP 2C8 and 3A4 and it does have active metabolites, and it is excreted in the urine and feces, primarily as metabolites and their conjugates.

Front 35

Alendronate

Back 35

It is not metabolized and because it is incorperated into bone, it has a very long half life ( > 10 years).

Front 36

Sulfamethoxazole/Trimethoprim

Back 36

Both metabolized by CYP 2C9 & 3A4.

Front 37

Lansoprazole

Back 37

Metabolized in the liver, mainly by CYP 2C19 and 3A4, and excreted in the urine and feces as metabolites.

Front 38

Clonazepam

Back 38

Metabolized in the liver via glucoronidation and sulfate conjugation. Also metabolized by CYP 3A4. It is excreted in the urine, mainly as metabolites.

Front 39

Tramadol

Back 39

Metabolized in the liver by CYP 2B6, 3A4, and 2D6. It has an active metabolite (O-desmethyl tramadol). And it is excreted in the urine, predominantly as metabolites.

Front 40

Levofloxacin

Back 40

Metabolism is minimal. It is excreted in the urine primarily as unchanged drug and it does undergo active tubule secretion.

Front 41

Fluoxetine

Back 41

Metabolized in the liver by CYP 2C19 and 2D6. It has an equally active metabolite (norfluoxetine). And it is excreted in the urine as both metabolites and unchanged drug.

Front 42

Prednisone

Back 42

Converted to prednisolone (the active metabolite) in the liver and it is a minor substrate for CYP 3A4.

Front 43

Omeprazole

Back 43

Metabolized in the liver by CYP 2C19 (mainly) and 3A4. It is excreted as metabolites in the urine (mainly) and the feces.

Front 44

Atenolol

Back 44

Limited metabolism in the liver. Excreted in the urine and feces.

Front 45

Insulin Glargine

Back 45

Metabolized to some extent (skin, liver, and kidney) and has 2 active metabolites. Excreted in the urine.

Front 46

Amoxicillin / Clavulanate

Back 46

Amoxicillin is excreted unchanged in urine, which is why the dosage is adjusted in cases of renal impairment. Clavulanate is metabolized in the liver and excreted in the urine.

Front 47

Fenofibrate

Back 47

Metabolized by esterases in the tissue and plasma to its active form, fenofibric acid, which is inactivated via glucuronidation in the liver and kidney. It is excreted as metabolites in the urine and feces.

Front 48

Celecoxib

Back 48

Metabolized in the liver by CYP 2C9. Excreted in the urine and feces.

Front 49

Donepezil

Back 49

Metabolized in the liver by CYP 3A4 & 2D6. Two of its four major metabolites are active. Both unchanged drug and metabolites are excreted in the urine (mostly) and feces.

Front 50

Ezetimibe & Simvastatin

Back 50

Simvastatin is a lactone prodrug. Hydrolysis of the lactone ring via carboxylesterases produces the active, beta-hydroxyacid form. Simvastatin undergoes extensive 1st pass metabolism via CYP3A4. The metabolites undergo biliary secretion, followed by excretion in the feces. Ezetimibe is glucuronidated in the small intestines and liver (has an active metabolite).

Front 51

Cephalexin

Back 51

Minimally metabolized. Excreted in the urine, mainly as unchanged drug.

Front 52

Mometasone

Back 52

Uses as an intranasal spray, systemic absorption is minimal and is not detectable in plasma, but mometasone is metabolized in the liver by CYP 3A4.

Front 53

Drospirenone & Ethinyl Estradiol

Back 53

Both are substrates of CYP 3A4.

Front 54

Vitamin D3

Back 54

Vitamins D2 and D3 are converted to 25-hydroxyvitamin D in the liver, which is then converted to 1,25-hydroxyvitamin D in the kidney.

Front 55

Ezetimibe

Back 55

Ezetimibe is glucuronidated in the small intestines and liver (has an active metabolite).

Front 56

Gabapentin

Back 56

Not metabolized. Excreted in the urine as unchanged drug.

Front 57

Pregabalin

Back 57

Minimally metabolized. Excreted in the urine, mainly as unchanged drug.

Front 58

Sildenafil

Back 58

Metabolized in the liver by CYP 3A4 (major) and CYP2C9. It does have an active metabolite. Excreted mainly in the feces.

Front 59

APAP/Codeine

Back 59

APAP is predominantly metabolized via conjugation with either sulfate or glucuronide. Minor pathways include metabolism via CYP 1A2 & 2E1. Metabolites are excreted in the urine. Codeine is metabolized predominantly by glucuronidation, via UGT2B7, in the liver, to form a comparably active metabolite. Codeine is also metabolized, to a more limited extent, via CYP 3A4, to another comparably active metabolite, and via CYP 2D6 to morphine, the most active metabolite. Codeine and its metabolites are predominately excreted in the urine.

Front 60

Fluconazole

Back 60

Excreted in the urine, primarily as unchanged drug.

Front 61

Intranasal Fluticasone

Back 61

Fluticasone is a substrate for CYP 3A4.

Front 62

Losartan

Back 62

Metabolized in the liver by CYP 2C9 & 3A4. It does have an active metabolite that is actually 40 times more potent than losartan itself.

Front 63

Propoxyphene-N/APAP

Back 63

APAP is predominantly metabolized via conjugation with either sulfate or glucuronide. Minor pathways include metabolism via CYP 1A2 & 2E1. Metabolites are excreted in the urine. Propoxyphen is metabolized by CYP 3A4 (major) and 2C9, and it does have an active metabolite, which is norpropoxyphen.

Front 64

Valacyclovir

Back 64

Valacyclovir is converted to acyclovir in the intestines and liver. It is excreted in the urine primarily as acyclovir (85%).

Front 65

Lorazepam

Back 65

Metabolized in the liver. Primarily excreted in the urine.

Front 66

Pantoprazole

Back 66

Metabolized in the liver by CYP 2C19 & 3A4. Excreted mainly in the urine (71%), but also in the feces (18%).

Front 67

Amlodipine/Benazepril

Back 67

Amlodipine is metabolized by the liver and excreted in the urine, predominantly as inactive metabolites. Benazepril is a prodrug. It is metabolized in the liver to its active metabolite, benazeprilat.

Front 68

Conjugated Estrogens

Back 68

Metabolized in the liver via CYP 3A4. Estradiol and estrone specifically are major CYP 1A2 & 3A4 substrates.

Front 69

Oseltamivir

Back 69

Metabolized in the liver to its active form, oseltamivir carboxylate. It does not interact w/ the cytochrome P450 system. It is excreted primarily in the urine, but also in the feces.

Front 70

Tiotropium

Back 70

Minimally metabolized in the liver by CYP 2D6 & 3A4.

Front 71

Aripiprazole

Back 71

Metabolized in the liver by CYP 2D6 & 3A4. Excreted in the urine and feces.

Front 72

Methylphenidate

Back 72

Metabolized by de-esterification to inactive metabolite, which is excreted predominantly in the urine.

Front 73

Digoxin

Back 73

Metabolized by either sugar hydrolysis in the stomach or via lactone ring reduction by intestinal bacteria. Digoxin is also a minor substrate for CYP 3A4.

Front 74

Fluticasone

Back 74

Fluticasone is a substrate for CYP 3A4.

Front 75

Fexofenadine

Back 75

Minimal metabolism. Excreted mainly in the feces, but also in the urine, as unchanged drug.

Front 76

Olmesartan

Back 76

The actual dosage form, olmesartan medoxomil, is a prodrug and is hydrolyzed in the GI tract to its active form, olmesartan. Olmesartan does not undergo further metabolism. Instead, it is excreted unchanged in the feces and urine.

Front 77

Pravastatin

Back 77

Metabolized in the liver and does have an active metabolite, 3-alpha-hydroxypravastatin, which has up to 10% of the activity of the parent drug. Pravastatin does not interact w/ any CYP enzymes.

Front 78

Triamterene/Hydrochlorothiazide

Back 78

Excreted as unchanged drug in the urine.

Front 79

Methylprednisolone

Back 79

Metabolized in the liver to inactive glucuronide and sulfate metabolites, which are excreted in the urine and feces.

Front 80

Cyclobenzaprine

Back 80

Metabolized in the liver by CYP 3A4, 1A2, and 2D6. Excreted in the urine, as inactive metabolites, and in the feces, as unchanged drug.

Front 81

Clonidine

Back 81

Metabolized in the liver. Excreted mainly in the urine.

Front 82

Risedronate

Back 82

It is not metabolized and because it is incorperated into bone, it has a very long half life ( > 10 years).

Front 83

Diazepam

Back 83

Metabolized in the liver, including metabolism by CYP 2C19 & 3A4. Excreted in the urine.

Front 84

Carisoprodol

Back 84

Metabolized in the liver by CYP 2C19 to meprobamate, which has anxiolytic and sedative effects. It is excreted in the urine as metabolites.

Front 85

Promethazine

Back 85

Metabolized in the liver, primarily by oxidation. It is excreted in the urine and feces.

Front 86

Memantine

Back 86

Excreted in the urine (up to 82% as unchanged drug).

Front 87

Potassium Chloride

Back 87

Excreted primarily in the urine, but also in the feces and through the skin.

Front 88

Citalopram

Back 88

Metabolized in the liver, mainly by CYP 3A4 & 2C19. It have active, but less potent, metabolites. Excreted in the urine.

Front 89

Meloxicam

Back 89

Metabolized in the liver by CYP 2C9 & 3A4. Excreted in the urine and feces as inactive metabolites.

Front 90

Latanoprost

Back 90

Metabolized via ester hydrolysis in the eye.

Front 91

Carvedilol

Back 91

Metabolized in the liver by CYP 2C9, 2D6, 3A4, & 2C19. It has 3 active metabolites. Excreted primarily in the feces.

Front 92

Oxycodone

Back 92

Metabolized in the liver by CYP 3A4 & 2D6. Some metabolites do have analgesic activity. Excreted in the urine.

Front 93

Paroxetine

Back 93

Metabolized in the liver by CYP 2D6. Excreted in the urine and feces.

Front 94

Olmesartan/Hydrochlorothiazide

Back 94

Olmesartan medoxomil is a prodrug and is hydrolyzed in the GI tract to its active form, olmesartan. Olmesartan does not undergo further metabolism. Instead, it is excreted unchanged in the feces and urine. HCTZ is excreted in the urine as unchanged drug.

Front 95

Tadalafil

Back 95

Metabolized by oxidation, followed by methylation and glucuronidation to clinically inactive metabolites. Biliary secretion leads to excretion in the feces as the main route of elimination (61%), though excretion in the urine is also significant (36%).

Front 96

Sitagliptin

Back 96

Minimally metabolized by CYP 3A4 & 2C8. Excreted mainly in the urine (87%), but also in the feces (13%).

Front 97

Ciprofloxacin

Back 97

Metabolized in the liver and excreted in the urine (mainly) and feces as both unchanged drug and metabolites.

Front 98

Amitriptyline

Back 98

Metabolized in the liver to nortriptyline, which is active, as well as other metabolites. Multiple CYP enzymes metabolize amitriptyline. It is excreted in the urine as glucuronide or sulfate conjugates of metabolites.

Front 99

Naproxen

Back 99

Metabolized in the liver and excreted primarily in the urine.

Front 100

Niacin ER

Back 100

Metabolized by the liver, where it undergoes extensive 1st pass metabolism, and excreted, primarily in the urine, as metabolites.

Front 101

Allopurinol

Back 101

Metabolized to active metabolites, mainly oxypurinol, and is excreted in the urine, primarily as oxypurinol.

Front 102

Losartan/Hydrochlorothiazide

Back 102

Losartan is metabolized in the liver by CYP 2C9 & 3A4. It does have an active metabolite that is actually 40 times more potent than losartan itself. HCTZ is excreted in the urine as unchanged drug.

Front 103

Tolterodine

Back 103

Metabolized in the liver by CYP 2D6 & 3A4. It has an active metabolite, 5-hydroxymethyltolterodine. It is excreted primarily in the urine, but also in the feces.

Front 104

Lisinopril/Hydrochlorothiazide

Back 104

Both lisinopril and HCTZ are excreted unchanged in urine.

Front 105

Norgestimate & Ethinyl Estradiol

Back 105

Ethinyl estradiol is metabolized by CYP 3A4. Norgestimate is metabolized in the liver. Both are excreted in the urine and feces.

Front 106

Penicillin VK

Back 106

Excreted in the urine as unchanged drug and metabolites.

Front 107

Codeine & Guaifenesin

Back 107

Codeine is a prodrug. Codeine is metabolized predominantly by glucuronidation, via UGT2B7, in the liver, to form a comparably active metabolite. Codeine is also metabolized, to a more limited extent, via CYP 3A4, to another comparably active metabolite, and via CYP 2D6 to morphine, the most active metabolite. Codeine and its metabolites are predominately excreted in the urine.

Front 108

Glyburide

Back 108

It is metabolized in the liver and some metabolites do have weak activity. It is excreted in the urine and feces equally.

Front 109

Fluticasone Inhaler

Back 109

Metabolized by CYP 3A4.

Front 110

Rabeprazole

Back 110

Metabolized in the liver by CYP 3A4 and 2C19. Mainly excreted in the urine (90%).

Front 111

Lisdexamfetamine

Back 111

Lisdexamfetamine is converted to dextroamphetamine via 1st pass intestinal and hepatic metabolism. CYP enzymes are not involved. Lisdexamfetamine was made a prodrug to decrease abuse potential as it is not effective if snorted or injected.

Front 112

Isosorbide Mononitrate

Back 112

Metabolized in the liver. Excreted primarily in the urine.

Front 113

Lamotrigine

Back 113

Metabolized in the liver and kidney, primarily via glucuronidation, to inactive metabolites.

Front 114

Olanzapine

Back 114

Metabolized via glucoronidation and by CYP 1A2 and 2D6. About 40% of the dose is removed by 1st pass metabolism. Clearance is increased by 40% in smokers and is decreased by 30% in females.

Front 115

Lovastatin

Back 115

Lovastatin is a lactone prodrug. Hydrolysis of the lactone ring via carboxylesterases produces the active, beta-hydroxyacid form. Lovastatin undergoes extensive 1st pass metabolism via CYP3A4. The metabolites undergo biliary secretion, followed by excretion in the feces.

Front 116

Ethinyl Estradiol & Etonogestrel Vaginal Ring

Back 116

Both are metabolized by CYP 3A4.

Front 117

Bupropion

Back 117

Metabolized by CYP 2B6, as well as by non-CYP processes, to metabolites, some of which are active. Metabolites can have up to as much as 50% of the activity of the parent drug. It is excreted primarily in the urine, but also in the feces, mainly as metabolites.

Front 118

Doxycycline

Back 118

Eliminated in the feces and urine as unchanged drug.

Front 119

Enalapril

Back 119

Enalapril is a prodrug. Cleavage of the ester group, in the liver, converts it to the active, diacid metabolite, enalaprilat. Metabolites are excreted mainly in the urine.

Front 120

Irbesartan

Back 120

Metabolized in the liver, mainly by CYP 2C9 and is excreted in the urine and feces.

Front 121

Amphetamine & Dextroamphetamine

Back 121

The enzymes involved in amphetamine metabolism have not been well defined. Renal elimination of amphetamine is highly pH dependent, w/ high pH resulting in less ionization and reduced renal elimination.

Front 122

Ibandronate

Back 122

Not metabolized.

Front 123

Eszopiclone

Back 123

Metabolized by CYP 3A4 and 2E1. Excreted predominantly in the urine, primarily as metabolites.

Front 124

Ipratropium & Albuterol Inhaler

Back 124

Albuterol: Excreted renally either as the parent compound or the primary metabolite. SULTIA3 (sulfotransferase) is thought to be the primary enzyme responsible for albuterol metabolism. Ipratropium is partially metabolized, primarily via hydrolysis and conjugation, to inactive metabolites. Approximately half of the dose is excreted unchanged in the urine.

Front 125

Folic Acid

Back 125

Metabolized in the liver. Excreted in the urine.

Front 126

Meclizine

Back 126

Metabolized in the liver. Excreted in the urine as metabolites and in the feces as unchanged drug.

Front 127

Ethinyl Estradiol & Norethindrone

Back 127

Ethinyl estradiol is metabolized by CYP 3A4. Norethindrone is metabolized by CYP 2C19 & 3A4.

Front 128

Buprenorphine & Naloxone

Back 128

Buprenorphine is partially metabolized by CYP 3A4 to norbuprenorphine. Both buprenorphine and norbuprinorphine undergo rapid glucuronidation. Buprenorphine and its metabolites are is excreted to a limited extent in the urine, but predominantly in the feces following enterohepatic circulation. Naloxone is metabolized in the liver, primarily via glucuronidation, and excreted in the urine.

Front 129

Raloxifene

Back 129

Raloxifene undergoes extensive 1st pass glucuronidation. The glucuronidated metabolites are secreted via bile into the intestines and then excreted in the feces.

Front 130

Omega-3-Acid Ethyl Esters

Back 130

Metabolized in the liver.

Front 131

Lidocaine Patch 5%

Back 131

Metabolized in the liver to a number of less active metabolites, which are excreted predominantly in the urine.

Front 132

Ramipril

Back 132

Ramipril is a prodrug. Cleavage of the ester group, in the liver, converts ramipril to its active, diacid metabolite, ramiprilat. Metabolites are excreted in the urine and feces.

Front 133

Benazepril

Back 133

Benazepril is a prodrug. Cleavage of the ester group, in the liver, converts benazeprill to its active, diacid metabolite, benazeprilat. Metabolites are excreted in the urine (mainly) and feces.

Front 134

Verapamil

Back 134

Verapamil undergoes extensive 1st pass metabolism. It is metabolized by CYP 3A4, 3A5, and 2C8. The main active metabolite of verapamil is norverapamil, which is further metabolized by CYP enzymes. It is excreted predominantly in the urine as metabolites.

Front 135

Ranitidine

Back 135

Metabolized by the liver and excreted in the urine.