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Pharmacology
Chapter 29
66
Pharmacology
Graduate
07/28/2014

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Term
Inability to maintain penile erection for the successful performance of sexual activity
Definition
erectile dysfunction
Term
organic & psychogenic causes, including sequelae to prostatic surgery
Definition
erectile dysfunction
Term
Erectile dysfunction previous therapies
Definition

penile implants

intrapenile injections of alprostadil

Term
Phosphodiesterase Type 5 (PDE5) Inhibitors
Definition

Sildenafil (viagra) first

Vardenafil (levitra) viagra me too

tadalafil (cialis) longest acting

Term
Physiologic mechanism of erection involves release of ____ in the corpus cavernosum during sexual stimulation
Definition
nitrous oxide (NO)
Term
What activates the enzyme guanylate cyclase?
Definition
Nitrous oxide
Term
Once enzyme guanylate cyclase is activated, it results in increased levels of...
Definition
cyclic guanosine monophosphate (cMP)
Term
cGMP produces
Definition
smooth muscle relaxation & inflow of blood to corpus cavernosum
Term
Parasympathetic muscarinic receptors activation results in.. (erection)
Definition
synthesis and release of NO from endothelial cells of blood vessels
Term
PDE5 inhibitors enhance the effect of NO by...
Definition

inhibiting phosphodiesterase type 5 which is responsible for degradation of cGMP

 

Term
how many PDE isoenzymes are there
Definition

11

PDE-6 in the eye

Term
Do not directly cause penile erections, but affects the response to sexual stimulation, no effect in absense of sexual stimulation
Definition
PDE 5 inhibitors
Term
Other therapeutic uses for PDE 5 inhibitors besides erection
Definition

pulmonary hypertension

benign prostatic hyperplasia

Term
which PDE 5 inhibitors work for pulmonary hypertension
Definition

silidenafil

tadalafil

Term
which PDE 5 inhibitor can be used for BPH
Definition

tadalafil

all three are effective but only tadalafil FDA approved

Term
Sil/Var should be taken PO, how long prior to anticipated sexual activity?
Definition
1 hour
Term
Benefits of PDE 5 inhibitors are observed for up to...
Definition
4 hours
Term
What is the duration of Tad?
Definition
18-36 hours
Term
PDE 5 inhibitors are rapidly absorbed by...
Definition

CYP3A4 

eliminated in bile

Term

Severe renal impairment, liver cirrhosis & older than 65

Decrease elimination

Definition
PDE 5 inhibitors
Term
Which drugs are contraindicated with nitrates
Definition
PDE 5 inhibitors
Term
Cation with alpha blockers with
Definition
PDE 5 inhibitors
Term
cation if anatomical deformation of penis with...
Definition
PDE 5 inhibitors
Term
PDE5 isozyme is found in...
Definition
vascular smooth muscle & platelets
Term
Adverse effects of PDE5 inhibitors
Definition

headache, flushing, dyspepsia, nasal congestions

mild decrased BP

cation with CVD (inherent risk of sex)

visual

Term
what are the visual adverse effects of PDE5 inhibitors
Definition
loss of blue/green discrimination (PDE6)
Term
Rare adverse effects of PDE5 inhibitors
Definition

rare eye condition, nonarteritic anterior ischemic optic neuropahty (NAION) has been associated PDE5 inhibitor use- CONTRAINDICATION

acute hearing los, sometimes accompanied by tinnitus & dizziness

Term
any disease process that results in reduction in the mass of bone per unit volume
Definition
osteoporosis
Term
Skeletal fragility with frequent bone fractures
Definition
osteoporosis
Term
Major cause of disability among the elderly
Definition
osteoporosis
Term
occurs predominantly in postmenopausal women, but also elderly of both sexes
Definition
osteoporosis
Term
Nondrug strategies for osteoporosis
Definition

diet with adequate Ca and Vit. D (not supplements)

weight-bearing exercise

cessation of smoking

Term
Bisophonates
Definition

Alendronate 

Ibandronate

Risedronate

Zoledronic acid

Term
MOA of biphosphonates
Definition
decreased osteoclastic bone reabsorption
Term
Bisphosphonate disorders of....
Definition

bone remodeling such as osteoporosis, Pagets disease

metastatic bone cancers

Term
Should be administered with 6-8 ounces of water at least 30 minutes to one hour (upright) before eating breakfast
Definition
biphosphonates
Term
Which drug has less than 1% absorbed
Definition
bisphosphonates
Term
Do not give if severe renal impairment
Definition
bisphosphonates
Term
Long terms of biphosphonates
Definition
unusual femur fractures, esophageal cancer, osteonecrosis of the jaw
Term
The first non-bisphosphonate anti-resorptive-blocks osteoclast activation
Definition
denosumab
Term
fully human monoclonal antibody
Definition
denosumab
Term
Route of administration of denosumab
Definition
injected subq once every 6 months
Term
Denosumab has increased risks of...
Definition

infection

secondary malignancies

hypocalcemia

dermatological rxns

Term
May be an effective alternative for high-risk patients who have not responded to bisphosphonates or cannot tolerate them
Definition
denosumab
Term
Other therapies for osteoporosis
Definition

HRT

Raloxifene

Calcitonin

Calcium

Teriparatide

Term
Hormone replacement therapy
Definition

estrogen replacement if no uterus

estrogen & progesterone if have uterus (caution)

Term
Raloxifene (therapy for osteoporosis)
Definition
SERM- selective estrogen receptor modulator
Term
Calcitonin
Definition

intranasal spray

inhibits bone reabsorption

Term
calcium
Definition
the institute of medicine recommends 1,200 mg/d in postmenopausal women (+ vitamin D)
Term
teriparatide (osteoporosis)
Definition

the 1-34 sequence of parathyroid hormone

increases bone formation

Term
Anorexic agents
Definition

phentermine (fastin)

lorcaserin hydrochloride

therapeutic claim (antiobesity, activate 5-HT2D)

Term
Lipase inhibitors
Definition
orlistat
Term

Presence of excess body fat

difficult to measure directly

 

Definition
obesity
Term
BMI
Definition

body mass index

weight in kg/ (height in meters)2

Term
Normal BMI
Definition
18.5-24.9
Term
overweight BMI
Definition
25-29.9
Term
class I obesity BMI
Definition
30-34.9
Term
Class II obesity BMI
Definition
35-39.9
Term
Class III extreme obesity BMI
Definition
> 40
Term
sympathomimetic amine
Definition
phentermine
Term
Amphetamine-like
Definition
phentermine
Term
Increased release of dopamine
Definition
phentermine
Term
Phentermine MOA
Definition

interfers in the reuptake of serotonin, dopamine & NE into the presynaptic nerve terminal thereby increasing their brain levels

direct stimulation of the satiety center in the hypothalmic & limbic regions

Term
Phentermine demographics
Definition

controlled schedule IV agents

increase HR and BP

dry mouth, headache, insomnia, conspipation

rarely pulm. hypertension

Term
Indications & uses for phentermine
Definition

BMI greater than or equal to 30

BMI greater than or equal to 27 in presence of other factors (HTN, DM, dyslipidemia) in conjunction with a reduced calorie diet

Term
Contraindications of phentermine
Definition

glaucoma

Hx of drug abuse

cardiovascular disease

moderate-severe hypertension

advanced arteriosclerosis

agitated states

within 14 days of MAOI administration

anorexia nervosa

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