PDE5s, anticholinergics, TCIs, Alpha-1 blockers, 5-alpha reductase inhibitors

Question 1

PDE5 inhibitor (phosphodiesterase type 5) vasodilator (-afil)

Answer 1

–Increases cGMP causing smooth muscle relaxation increasing blood flow to the penis (guanosine 3’, 5’-cyclic monophosphate regulates cell functioning)
–Need to monitor blood pressure (BP) and CrCl (Creatine) levels (renal [kidney] function)

Question 2

PDE5 INHIBITOR indications

Answer 2

–Erectile dysfunction (ED)\ Sexual dysfunction in women
–Pulmonary arterial hypertension (HT of the lungs)
–Sexual dysfunction due to antidepressants

Question 3

PDE5 INHIBITOR contraindications

Answer 3

–Nitrates (esp. drugs like nitroglycerin)
–Fluconazole
–Alpha blockers (-osin)
–Liver disease
–Heart conditions (esp. angina)
–Renal (kidney)/Hepatic (Liver) impairment will require lower doses

Question 4

PDE5 INHIBITOR side-effects

Answer 4

–Flushing
–Dyspepsia (indigestion)
–Headache (HA)
–Diarrhea
–Myalgia (muscle weakness)
–Tiredness
–Blurred vision

Question 5

PDE5 INHIBITOR adverse effects

Answer 5

–vision loss (can be temporary or permanent)
–priapism over 4 hours

Question 6

PDE5 INHIBITOR foods to avoid

Answer 6

–High in nitrates: caffeine, cured meats/deli meats
–Grapefruit

Question 7

Levitra (vardenafil): PDE5 inhibitor

Answer 7

–Indication: ED
–AR: 2 hours
–BA: 15%
–1/2 Life: 4 hours

Question 8

Viagra (vardenafil): PDE5 inhibitor

Answer 8

–Indication: ED
–AR: 30–120 minutes
–BA: 40%
–1/2 Life: 4 hours

Question 9

Cialis (tadalafil): PDE5 inhibitor

Answer 9

–Indication: ED
–AR: 2 hours
–BA: 88%
–1/2 Life: 17.5 hours

Question 10

ANTICHOLINERGIC (ANTIMUSCARINIC)

Answer 10

–Inhibits action of acetylcholine to relax smooth bladder muscles (stops the Ca+ channel gate by binding to the muscarinic receptor) muscarinic receptor antagonist
–Muscarinic acetylcholine receptors exist on the smooth muscle of the organs

Question 11

ANTICHOLINERGIC (ANTIMUSCARINIC) indication

Answer 11

Overactive bladder (incontinence)

Question 12

ANTICHOLINERGIC (ANTIMUSCARINIC) contraindications

Answer 12

–Narrow angle glaucoma (increased eye pressure)
–Urinary retention
–Gastric retention

Question 13

ANTICHOLINERGIC (ANTIMUSCARINIC) side effects

Answer 13

–Dizziness
–Drowsiness (especially with Ditropan (oxybutynin))
–Xerostomia (dry mouth)
–Constipation
–Urinary retention
–Agitation
–Blurry vision

Question 14

ANTICHOLINERGIC (ANTIMUSCARINIC) foods to avoid

Answer 14

–grapefruit
–drinks with excessive caffeine

Question 15

ANTICHOLINERGIC (ANTIMUSCARINIC) medications to avoid

Answer 15

–Potassium supplements
–Antifungal (increases elimination)

Question 16

Vesicare (solfenacin succinate): anticholinergic (antimuscaric)

Answer 16

–Indication: overactive bladder
–AR: 3–8 hours
–BA: 88%
–1/2 Life: 45–68 hours

Question 17

TRI-CYCLIC ANTIDEPRESSANTS (TCI)

Answer 17

–First line antidepressants in the 1950s
–Second-line antidepressants to SSRI (selective serotonin reuptake inhibitor)
–TCIs block the reuptake of serotonin and norepinephrine

Question 18

TRI-CYCLIC ANTIDEPRESSANTS indications

Answer 18

–Manage depression
–Childhood enuresis (bedwetting)
–Low back pain
–Off-label use: cocaine dependance, ADHD, panic disorder, urinary incontinence, bulimia nervosa, migraines, neuralgia (nerve pain)

Question 19

TRI-CYCLIC ANTIDEPRESSANTS side-effects

Answer 19

–Blurry vision
–Constipation
–Xerostomia (dry mouth)
–Orthostatic hypotension (lightheadedness standing too quickly)
–Weight loss (appetite increase)/ Weight gain (increase appetite)
–Tremors
–Low libido

Question 20

TRI-CYCLIC ANTIDEPRESSANTS adverse effect

Answer 20

–Suicidal tendencies in children and adolescences

Question 21

TRI-CYCLIC ANTIDEPRESSANTS foods to avoid

Answer 21

–Anything high in tyramine (amino acid that has peripheral cardiac effects) these foods can elevate blood pressure, avoid at least 2 weeks after stopping medication
–Organ meats (liver, kidneys, heart, etc.), poultry, fish
–Citric fruits, especially grapefruit
–Pickled foods: sauerkraut, kimchi, beets, cucumbers, peppers
–Tofu, miso, soy sauce
–Decaffeinated coffee, alcohol
–Avoid St. John’s Wart supplement

Question 22

Tofranil (imipramine): TCI

Answer 22

–Indication: Anti-depressant
–AR: 2–8 hours
–BA: 40–50%
–1/2 Life: 31–46 hours

Question 23

5-ALPHA REDUCTASE INHIBITOR

Answer 23

–Converts testosterone to dihydrotestosterone reducing the DHT level shrinking the prostrate
–Take with or without food avoid alcohol and grapefruit juice
–Avoid BP medications especially Alpha-1 blockers (-osin)
–Topical 15 times more effective (scalp, shampoos)

Question 24

Avodart (dutasteride): 5-Alpha reductase inhibitor

Answer 24

–Indications: Benign prostatic hyperplasia (BPH), androgenic alopecia
–AR: 2–3 hours
–BA: 60%
–1/2 Life: 5 weeks

Question 25

Proscar (finasteride): 5-Alpha reductase inhibitor

Answer 25

–Indications: BPH, androgenic alopecia –AR: 6–8 hours –BA: 65% –1/2 Life: 4–5 days

Question 26

UROXATRAL (ALFUZOSIN) ALPHA-1 BLOCKER (-OSIN)

Answer 26

–Relaxes muscles of the bladder/prostrate –Reduces blood pressure by blocking the alpha-1 adrenoceptor which blocks the calcium channel gate (epinephrine, norepinephrine) relaxing smooth muscles –Taking garlic or ginseng supplements can decrease the effect –Limit alcohol –Avoid caffeine and grapefruit –Avoid exercising in hot weather or standing for long periods of time –Avoid other alpha blockers and ED medications (sildenafil, tadalafil, vardenafil), anti-fungal

Question 27

UROXATRAL (ALFUZOSIN) ALPHA-1 BLOCKER (-OSIN) side-effects

Answer 27

–Orthostatic hypotension (low BP standing up quickly) –Syncope (fainting) lightheadedness or dizziness –Runny nose –Headache –Heartburn, stomach pain –Nausea –Constipation –priapism (rare)

Question 28

UROXATRAL (ALFUZOSIN) ALPHA-1 BLOCKER (-OSIN) adverse effects

Answer 28

–Damage blood vessels in brain, heart, kidneys, –Increased risk of stroke/HA, irregular heartbeat

Question 29

Uroxtral (alfuzosin): Alpha-1 blocker

Answer 29

–Indications: HT, BPH –AR: 8 hours –BA: 49% –1/2 Life: 10 hours