Exam 4 - Sexxx Flashcards
Sex Pharm
Limitations
1) taboo
2) animal studies hormonal > brain
2) male focus
Factors Affecting
Sexual Activity
1) Physical/Mental Health
2) Hormone status, mood circumstance
3) Psych conditioning, expectations
4) Drug use
Libido
Sex drive (hypothalamus, limbic/reward system)
Performance
Male: erection, ejactulation
Female: lubrication, organsm
Hormones & NTsthat increase
libido include:
1) testosterone (male/female)
2) dopamine
3) estrogen? (females)
4) LH/FSH?
Hormones & NTs that
decrease libido:
1) prolactin (male/female)
2) estrogen (male)
3) serotonin
4) progesterone?
How do DA receptor agonists
& antagonist effect libido?
DA agonists ^^ libido
DA antagonist vv libido
How do alpha 2 blockers effect
libido?
^ libido by ^ NEpi in synapse
How do beta blockers & alpha
2 agonists effect libido?
decrease libido
How do nicotinic agonists
effect libido?
may ^ libido by enhancing DA
release
How do muscarinic antagonists
affect libido?
decrease libido
How does serotonin (5-HT)
effect libido?
decrease libido
Male Sexual Response:
parasympathetic
1) penile engorgement & erection
2) closure of bladder neck
Female Sexual Response:
parasympathetic
1) clitoral erection
2) lubrication
Male Sexual Response:
sympathetic
1) seminal emission
2) ejactualtion
2) detumescence (de-erection)
Female Sexual Response:
sympathetic
1) contraction of uterus, vagina,
fallopian tubes
Male Sexual Response:
somatic
erection and orgasm contribution
Female Sexual Response:
somatic
contribution to orgasm
Typical mechanisms for drug
related decreased libido:
1) increased prolatin secretion
2) anti-androgenic effect
3) block DA, NE, orAch
4) sedation
5) enhance 5-HT
Typical mechanisms for drug
interference w erection:
1) peripheral anti-muscarinic action
2) decreased blood flow
Typical mechanisms for drug
interference of orgasm:
1) alpha 1 blockade
2) local anethetic
3) sedative effects
Anti-HTNs with high incidence
of sexual dysfunction:
1) ganglionic blockers
2) Clonidine & methyldopa
3) alpha 1 blockers
4) beta blockers
Ganglionic blockers cause:
complete failure of erection and orgasm
Clonidine & methyldopa cause:
decreased libido and impotence via
sympatholytic effects
Alpha 1 blockers cause:
^incidence of ejaculatory failure
no erection effect
Beta blockers cause:
5 - 10% incidence of ED
lower libido reported
Spironolactone causes:
decreased libido and frequent
impotence
MOA of spironolactone
sexual dysfunction:
1) blocks DHT from receptor
2) inhibits 5 alpha reductase (testosterone)
3) ^prolactin
Thiazide diuretic induced
sexual dysfunction:
1) 5 - 30% incidence
2) impotence
3) vv libido
4) difficult ejaculation
* MOA uncertain
Anti-HTNs with fewer side
effects include:
1) Ca channel blockers
2) ACE inhibitors
3) ARBS
4) direct renin inhibitors
Antipsychotics vv libido by:
1) DA block
2) CNS anticholinergic effect
3) CNS sedative effect
Antipsychotics cause ED by:
peripheral anticholinergic effects
Antipsychotics cause problems
with orgasm by:
alpha 1 blockade
Do “atypical” psychotics have more
or less sexual dysfunction effects?
less
SSRIs and sex:
1) vv libido (30-50%)
2) difficult orgasm
3) vv compliance do to sexual side effect
Trycyclics and sex:
1) impotence
2) vv lube (anticholinergic)
3) impaired orgasm (alpha 1 block)
4) enhanced serotonin(vv libido)
MAOIs and sex:
1) difficult organsm
2) ejaculatory failure (phenelzine)
Antidepressants w fewer
side effects:
1) bupropion
2) mirtazapine
3) vilazodone
4) trazodone
bupropion sexual side effects:
enhanced libido reports (DA?)
Mirtazapine (allpha 2 blcoker)
sexual side effects:
may ^ libido but also highly sedative
Trazodone sexual side effects:
mixed reports (^libido but anorgasm amd rarely priapism) * also highly sedative
Benzodiazepine sexual
side effects:
1) sedation
2) delayed orgasm
3) ejaculatory failure
Antiseizure med sexual side
effects:
SOME assoc w decreased libido
& performance difficulty
Which antiseizure med ^ libido?
ethosuximide
Which drug vv libido by ^prolactin
& estradiol?
cimetidine
How do opioids vv libido?
^ prolactin
Important to not with
recreational drugs:
1) acute & chronic effects differ
2) dose related differences
Acute effects of alcohol:
1) small dose: disinhibiting, ^libido,
2) ^dose: delayed or diminished orgasm
Chronic effects of alcohol:
1) neuropathy related impotence
2) vv testosterone (low libido, vv secondary
sex characteristics
Acute marijuana effects:
1) low dose: enhanced sensory, disinhibition, ^empathy
2) ^dose: impotence, anxiety
Chronic marijuana effects:
1) vv spermatogenesis
2) vv testosterone (low libido, impotence),
irregular menses, anovulation
Acute cocaine effects:
1) low dose: ^DA (^libido), delayed orgasm
2) ^dose: direct stim of erection
Chronic cocaine effects:
1) loss of libido
2) ejaculatory failure
Acute opiod effects:
^sexual activity may be do to
disinhibition
Chronic opiod effects:
1) low libido (2/3)
2) ED (1/2)
3) ejaculatory delay (2/3)
LSD and sex:
^sensory
MDA (ecstacy) and sex:
^sexual feelings and empathy
PCP and sex:
Not assoc w sexual activity.
vv sensation, depression, psychosis
Premature ejaculation tx:
1) local anesthetic
2) other experimented agents also
vv libido (clomipramine, thioridazine, MAOIs, benzos)
Testosterone uses:
1) vv gonadal fx
2) ^libido in men and women (lower dose)
testosterone side effects:
1) may accelerate prostate cancer
2) atherosclerosis?
What are some dopamine
antagonists?
1) L-DOPA
2) bromocriptine
3) ampomorphine
4) methylphenidate (Ritalin)
5) buproprion (wellbutrin)
L-DOPA uses:
Parkinson’s antecdote
Prolactinemia tx:
bromocriptine
ED folk remedies:
stimulants (kava, coca, strychnine),cannabis,betel nuts,bear gall bladder,rhino horn, ginseng, yohimbine
- most ineffective
Yohimbine ED txs
1) current rx: yocon, erex
2) MOA: alphpa 2 antagonist
3) effects: ^libido, ED improved
4) efficacy: uncertain
Yohimbine side effects:
nausea, sweating, tremor, ^BP&HR,
anxiety, irritability
Smooth muscle relaxants used
to tx ED include:
1) papverine
2) phentolamine
3) prostaglandin E
Adverse effects of papaverine:
bradycardia, HoTN, priapism,
hepatotoxicity, penile fibrosis
Phentolamine ED MOA:
alpha 1 blocker
(blocks symp smooth muscle contraction)
*papaverine adjunt, may interfere w orgasm
How is prostaglandin E
administered for ED?
injection or urethral suppository
Adverse effects of
prostaglandin E include:
HoTN, penile pain, ocassional priapism
Phosphodiesterase Inhibitors
used to tx ED include:
1) sildenafil (viagra)
2) avanafil (stendra)
3) vardenafil (levitra)
4) tadafil (cialis)
Viagra ADME:
1) peak conc @ 1 hr
2) 4 hour half life
3) ~ 4 hr duration
Peak conc avanafil:
30 - 45 min
Peak conc vardenafil:
30 min - 2 hrs
effective4 hrs, half life4-5 hrs
peak conc tadalafil:
1 - 6 hrs
effective 36 hrs, half life 18 hrs
BPH tx:
cialis (tadafil)
* avoid alpha blockers when taking cialis
Pulmonary HTN tx:
revatio (sildenafil)
*sxs & exercise capacity improved
Adverse effects of PDE inhibitors:
Common: HoTN, headache, flushing,indegestion
Less common: visual disturbances, acute
hearing loss, nasal congestion, rash,
diarrhea
How are PDE inhibitors
metabolized?
CYP3A4
What are the adverse effects of
PDE inhibitors and nitrates?
BP drop, syncope, lower cardiac perfusion,
MI (128 in deaths in first 8 months of use)
What is the MOA for ED drugs?
relaxation of smooth muscle in
corpora cavernosa
Estrogen uses:
1) vaginal atrophy, dryness, dyspareunia
2) libido?
3) helpful in menopause
Low lidido tx for women:
androgen/testosterone patch may
enahnce libido and satisfaction
Osphena MOA:
selective (vaginal) estrogen receptor modulator
Female effects of sildenafil
may include:
genital engorgement
limited success
Tx of female sexual dysfunction:
1) DA agonists (libido)
2) bupropion (DA enhancer)
3) alprostadil (PGE cream)
4) phenotolamine (alpha blocker)
5) neutraceuticals, filbanserin, bremelanotide(experamental)
Filbanserin MOA:
5-HT agonist, 5-HT2 antagonist
development on hold
Bremelanotide MOA:
1) melanocortin synthetic / alpha MSH
2) centrally stim libido male & female
3) original nasal spray withdrawn
4) subcutaneous formula in trials
