SEXUAL
PHARMACOLOGY
Susan J Campling, RN, Psy.D
Director of Special Projects
Pine Grove Behavioral Health
Hattiesburg MS 39402
In the very act of giving, I experience my
strength, my wealth, my power. This experience
of heightened vitality and potency fills me with
joy.
Erich Fromm, The Art of Loving
Objectives
• Understand the relationship between common
medications and sexuality including hyper-sexuality
• Identify relevant brain structures, chemistry, and
processes inherent to sexuality
• Discuss ethical considerations related to this discussion
Ethical Considerations
• Potential for abuse/ addiction
• Forced sterilization/ impotence
• Lack of informed consent for patients
• Potential for social abuse
• Who gets these medications?
• ED medications, birth control, anti androgens
• Potential for clinician prejudices
• Lack of research with women
• Information overload
Haroutunian Imperative
“Every addiction presentation must have
at least one brain slide.”
Localized Sex Brain Activity
• Cerebral cortex- all cortical regions
• Temporal parietal regions- important for integrating
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information and abstract concepts
Anterior insula (c) - reflect on the state of our bodies,
memory
Hippocampus-manages our memories
Septum-located near amygdala; smell activation;
pleasure
Amygdala- (sc)orchestrates powerful emotions
Nucleus acumens (sc)- pleasure , cognition and motor
functions
Striatum (sc)- reward but also averse, novel intense
stimuli
Brain Region of the Day
The Insula!!!
Insular Cortex
• Sensation of pain is judged for intensity and quality
• Area where pain is judged through imagination
• IBS – abnormal processing of visceral pain
• Empathy and compassion
• Perception of a full bladder and abdominal distention
• Sensation of non-painful warmth and coldness
• Homeostasis is controlled via autonomic functions
through the regulation of the sympathetic and
parasympathetic systems.
• Bodily self-awareness
• Sense of agency and body ownership
• Processes a person's sense of disgust both to smells and
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to the sight of contamination and mutilation— even when
just imagining the experience
Orgasm
Integration of information relating to bodily states into
higher-order cognitive and emotional processes
Larger in people who meditate
Activated when drug abusers are exposed to
environmental cues that trigger cravings; people, places
and things
Body memories? Anticipation butterflies in stomach
Maternal love and romantic love are more alike than lust yet there is significant
over- lap.
Ivanka Savic and Per Linstrom, Stockholm Brain Institute, April 2008, Pet and
MRI Differences in cerebral asymmetry and functional conductivity between
homo and heterosexual subjects
Direct Side Effects
• Anorgasmia
• Sex drive disorders
• Dyspareunia
• Anesthetic orgasm
• Retrograde ejaculation
• Priapism
• Gynecomastia
• Clitoral hypertrophy
Direct Side Effects
• Infertility/ sterility
• Hormonal-
gynecomastia,
hypogonadism
• Menstrual disorders
What is priapism?
Indirect Side Effects
• Body image
• Comfort
• Odors/ taste alteration
• Gastrointestinal side
effects
• Urinary tract
• Neurological
• Cardiovascular
• Skin
• Sensory impairment
FYI
• Agonist stimulate and facilitate a response in a pathway
• Antagonist act against the pathway
a
Alpha 1 Adrenergic
• Enhance desire and
• Needed for starting the
arousal
• Promotes peripheral
vasoconstriction (dose
dependent)
• Facilitate dopamine,
testosterone,
acetylcholine,
vasopressin,
prostaglandins
• α receptors fight flight
response
• Norepinephrine
engine but too much
leads to premature
ejaculation and
impotence
• Epinephrine/ norepi pass
through
• Doxazosin- Cardura-
antagonist
Alpha 2 Andrenergics
• Decrease desire and
• Clonidine-
sexual arousal
• Prompts
vasoconstriction
antagonizes alpha 1
activity
• Can decrease anxiety
related premature
ejaculation
• Can also cause
impotence
• agonist 
• Yohimbine• antagonist 
Bonus Question
What is lordosis?
Beta 2 Andrenergic Activity
• Smooth muscle dilation
• Pulmonary Vasodilator
• Promotes performance
anxiety
• Part of fight flight response
• Albuterol- agonist
• Labetalol (Trandate)-
antagonist
• Atenolol- β 1 antagonist
GABA
• Sedating
• Reducing anxiety and panic
• Diminishes active sexual
response
• Promotes lordosis
• Valium and Xanax stimulate
GABA receptors
• Alcoholism, the GABA system
is down-regulated and the
neuron may eventually become
dependent on alcohol to enable
GABA to function.
Excitatory
Biochemistry
• Cholinergic (acetocholine)- stimulate theta
waves; mediates all types of sexual thoughts,
attitudes and memories; limbic; hippocampus
• Cortisol (acute)- high levels associated with
psychoses, derangement, aggression
• Cortisol (chronic)- decreased sex drive to bizarre
psychotic behavior
• DHEA/ DHEAS- most abundant androgen
• Dopamine- pleasure, increase sex drive,
promotes orgasm
Excitatory
• Testosterone
• Zinc- needed for spermatogenesis: reduces GABA and
endogenous opioids
• Estrogens- essential to female desire, attraction,
lubrication orgasm, satisfaction,
• Histamine
• Oxytocin/ vasopressin*
Inhibitory
• Estrogen- men baldness and Gynecomastia
• Melatonin- causes gonadal recession in animals
• MAO- breaks down monoamines (NE, E, 5-HT,
DA) MAO B enzymes break down DA and phenyl
ethylamine (PEA)
• Opioids-most powerful sexual inhibitory
neurotransmitter; testosterone decreased in male
opiate addicts
Progesterone- “anti-aphrodisiac”
Prolactin- elevated levels in nursing
mothers; reduces sex drive in both men
and women
Serotonin-restrains excessive
excitement
Thyroid- sub therapeutic deceases sex
drive and is associated with depression;
elevated is toxic to tissue metabolism
Drugs and Medical Conditions that are Associated
with Hypersexuality
Stimulants
Cocaine, Adderall, Ritalin,…
• Generally thought to enhance libido
through increased sexual pleasure and
endurance
• Increased autoerotic behaviors
• Can cause psychotic states and sexual
deviance
• http://www.cdc.gov/hiv/resources/factshee
ts/meth.htm
(Everett H. Ellinwood, M.D.,
George King, Ph.D. and Tong H. Lee, M.D. Ph.D.)
Dopamine Agonists
Medications
• Parlodel (bromocriptine)
Conditions
• Dopamine deficiency
• Dostinex (cabergoline)
• Permax (pergolide; no
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longer used in US)
Mirapex and Sifrol
(pramipexole)
Requip (ropinirole)
Apokyn (apomorphine)
Neupro (rotigotine)
Norprolac (quinagolide)
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syndromes;
Parkinson’s Disease
Prolactinoma
Restless leg syndrome
Research on use in IVF
Anxiolytics
Benzodiazepines
• Increases GABA,
progesterone,
cholinergic activity
• Decreases
testosterone, cortisol,
serotonin
• Is associated with
hyper-sexuality
• Xanax, Librium,
Klonopin, Ativan
• Bus Par*- 5HT agonist-
does not impact
GABA; some research
suggests decreased
paraphilia fantasy and
transvestic fetishism
(Federoff, 1992)
Antidepressants
MAO
MAOIs
• Marplan
• Nardil
• Parnate
• Side effects include
erectile dysfunction,
orgasms diminished,
ejaculation retarded
• Can treat hyper
sexuality
• Have a lot of dietary
restrictions
• A lot of medication
restrictions
Antidepressants
SSRI
• Increased cortisol
• Clomipramine-
• Increased opioids
Anafranil
• Fluoxetine- Prozac
• Fluvoxamine- Luvox
• Paroxetine- Paxil
• Sertraline- Zoloft
• Venlafaxine- Effexor
• Trazadone-hybridsex drive; priapism
• Increased prolactin
• Increased 5-HT
• Associated with hypo
sexuality and hyper
sexuality
• Retarded ejaculation
• Anorgasmia/
spontaneous orgasm
Bupropion
• Novel antidepressant
• Does not generate
• Side effects tend to be
sexual stimuli but
reinforces stimuli that
is already occurring
• Increases DHEAS in
women which may
have an anti-aging
effect
• Psychosis risk
• Hyper-sexuality rare
activating
• Preferred when
depression is present
but not anxiety
• Actives limbic system
• Influences areas
where orgasm arises
Oxytocin and Vasopressin
• Oxytocin-coitus, birth,
breastfeeding; increases
male fantasies; makes skin a
sexual organ (female),
dissociative
• Vasopressin-antidiuretic
hormone; increases
cognition and memory
• LHRH-high dose lowers
testosterone (SO)
• Pulsating dose- testes
size; nocturnal emissions;
spontaneous erections
DHEA/ DHEAS
Adrenergic
• DHEAS- precursor to
• Promotes weight loss
estrogic and androgenic
steroids
• May be metabolized into
sexual pheromone
substances in the skin and
involved in sexual
attraction through touch
and smell
• DHEA rhythmic
• DHEAS constant diurnal
levels
• Promotes bone growth
• No consistent research to
indicate increased sexual
response except in
females with adrenal
insufficiency
• Study 2010 demonstrated
increased DHEA-S levels
in women when viewing
sexual and humorous films
but not anxiety invoking
movies
Hormones- Male Inhibitory
• Cyproterone-(Androcur)-? decreased sexual
fantasies, behavior, masturbation, intercourse and
erection
• Medroxyprogesterone (Provera)- decreased libido,
sexual arousal, fantasies, urges and behaviors
• Leuprolide (Lupron) LH- decreases testosterone and
estrogen
• Goserolin (Zoladex) LH- decreased testosterone and
estrogen
• Cimetidine- Tagamet (has slight anti-androgen
effects)
Antipsychotic/Neuroleptics
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Chlorpromazine-Thorazine
Fluphenazine-Prolixin
Mesoridazine-Serentil
Haloperidol- Haldol
Risperidone- Risperdal
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Valproic Acid (ac)- Depakote
Carbamazepine- Tegretol
Phenytoin- Dilantin
Phenobarbital-
What over the counter GERD
medication may have androgen
properties?
• Hypo sexuality/ hyper
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sexuality (rare)
Priapism
Anorgasmia
Orgasm without ejaculation
Anesthetic orgasm
May be useful for hyper
sexuality
• Anticonvulsant medications
impact hormonal regulation
and generally decrease
sexual desire
Miscellaneous
• Opioid Antagonists-Naltrexone- some early + studies,
kleptomania, trichotillomania ,internet porn or
pathological gambling. Vivitrol marketed for alcohol.
• Cold medication- Mucenex DM- MD synthetic
morphine
• Asthma- Beta 2 agonists (albuterol, epinephrine
Primatene), xanthines (theophylline, caffeine over
reactivity), corticosteroids (HPA; paranoia,
depression, aggression), anticholinergic (atrovent)
dry mouth and vagina.
Yohimbine
• Inhibits platelet
• Avoid with panic/
aggregation
• Acts as a stimulant
• Desire enhanced
• Positive effects on
erection and
ejaculation
• Synthetic and herbal
forms
anxiety
• Sexual obsessions and
compulsions
• Sexual phobias
• Combination
formulations –Zumba
ED Medications
• Do not enhance desire
directly, utilizes nitric
oxide, a penile
vasodilator substance,
enhances
responsiveness to
stimuli, can cause
deafness, not to be
used with nitrates
• Cialis, Viagra, Levitra
Medical Conditions
• MS
• Tumors-hypothalamic, frontal cortex, temporal lobes,
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septal nuclei, etc.
TBI
Nero syphilis
Mania
Kleine Levine-Sleeping Beauty Syndrome
Fetal alcohol and PDD
Epilepsy
Summary
• Human sexuality is a complex process that can be
impacted by multiple direct and indirect medication effects
• Our understanding of the structures associated with
sexual responses is an evolving process
• Research is needed with women and GLBT around the
physiology of sexuality