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Sexual Pharmacology . Susan J Campling, RN, Psy.D Director of S pecial 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.

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sexual pharmacology

Sexual Pharmacology

Susan J Campling, RN, Psy.D

Director of Special Projects

Pine Grove Behavioral Health

Hattiesburg MS 39402

slide2

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
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
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
HaroutunianImperative

“Every addiction presentation must have

at least one brain slide.”

localized sex brain activity
Localized Sex Brain Activity
  • Cerebral cortex- all cortical regions
  • Temporal parietal regions- important for integrating 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
insular cortex
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.
slide10

Bodily self-awareness

  • Sense of agency and body ownership
  • Processes a person\'s sense of disgust both to smells and 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
slide12

IvankaSavic 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
Direct Side Effects

Back to medications

  • Anorgasmia
  • Sex drive disorders
  • Dyspareunia
  • Anesthetic orgasm
  • Retrograde ejaculation
  • Priapism
  • Gynecomastia
  • Clitoral hypertrophy
direct side effects1
Direct Side Effects
  • Infertility/ sterility
  • Hormonal- gynecomastia, hypogonadism
  • Menstrual disorders

What is priapism?

indirect side effects
Indirect Side Effects
  • Body image
  • Comfort
  • Odors/ taste alteration
  • Gastrointestinal side effects
  • Urinary tract
  • Neurological
  • Cardiovascular
  • Skin
  • Sensory impairment
slide17
FYI
  • Agonist stimulate and facilitate a response in a pathway
  • Antagonist act against the pathway

a

alpha 1 adrenergic
Alpha 1 Adrenergic
  • Enhance desire and arousal
  • Promotes peripheral vasoconstriction (dose dependent)
  • Facilitate dopamine, testosterone, acetylcholine, vasopressin, prostaglandins
  • α receptors fight flight response
  • Norepinephrine
  • Needed for starting the engine but too much leads to premature ejaculation and impotence
  • Epinephrine/ norepi pass through
  • Doxazosin- Cardura-antagonist
alpha 2 andrenergics
Alpha 2 Andrenergics
  • Decrease desire and sexual arousal
  • Prompts vasoconstriction antagonizes alpha 1 activity
  • Can decrease anxiety related premature ejaculation
  • Can also cause impotence
  • Clonidine-
  • agonist 
  • Yohimbine-
  • antagonist 
what is lordosis

Bonus Question

What is lordosis?

Beta 2 Andrenergic Activity

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.

  • Smooth muscle dilation
  • Pulmonary Vasodilator
  • Promotes performance anxiety
  • Part of fight flight response
  • Albuterol- agonist
  • Labetalol (Trandate)- antagonist
  • Atenolol- β 1 antagonist
excitatory biochemistry
ExcitatoryBiochemistry
  • 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
Excitatory
  • Testosterone
  • Zinc- needed for spermatogenesis: reduces GABA and endogenous opioids
  • Estrogens- essential to female desire, attraction, lubrication orgasm, satisfaction,
  • Histamine
  • Oxytocin/ vasopressin*
inhibitory
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
slide25

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
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 (Everett H. Ellinwood, M.D., George King, Ph.D. and Tong H. Lee, M.D. Ph.D.)
  • Can cause psychotic states and sexual deviance
  • http://www.cdc.gov/hiv/resources/factsheets/meth.htm

Why would stimulants possibly lead to

impotence?

dopamine agonists
Dopamine Agonists

Medications

Conditions

Dopamine deficiency syndromes;

Parkinson’s Disease

Prolactinoma

Restless leg syndrome

Research on use in IVF

  • Parlodel (bromocriptine)
  • Dostinex (cabergoline)
  • Permax (pergolide; no longer used in US)
  • Mirapex and Sifrol (pramipexole)
  • Requip (ropinirole)
  • Apokyn (apomorphine)
  • Neupro (rotigotine)
  • Norprolac (quinagolide)

Anything that floods D into what

brain structure can become addictive?

anxiolytics
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
AntidepressantsMAO

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
AntidepressantsSSRI
  • Increased cortisol
  • Increased opioids
  • Increased prolactin
  • Increased 5-HT
  • Associated with hypo sexuality and hyper sexuality
  • Retarded ejaculation
  • Anorgasmia/ spontaneous orgasm
  • Clomipramine- Anafranil
  • Fluoxetine- Prozac
  • Fluvoxamine- Luvox
  • Paroxetine- Paxil
  • Sertraline- Zoloft
  • Venlafaxine- Effexor
  • Trazadone-hybrid-sex drive; priapism
bupropion
Bupropion
  • Novel antidepressant
  • Side effects tend to be activating
  • Preferred when depression is present but not anxiety
  • Actives limbic system
  • Influences areas where orgasm arises
  • Does not generate 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
oxytocin and vasopressin
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
DHEA/ DHEASAdrenergic

Available OTC

  • DHEAS- precursor to 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 weight loss
  • 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
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
Antipsychotic/Neuroleptics
  • Chlorpromazine-Thorazine
  • Fluphenazine-Prolixin
  • Mesoridazine-Serentil
  • Haloperidol- Haldol
  • Risperidone- Risperdal
  • Valproic Acid (ac)- Depakote
  • Carbamazepine- Tegretol
  • Phenytoin- Dilantin
  • Phenobarbital-
  • Hypo sexuality/ hyper 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

What over the counter GERD medication may have androgen properties?

miscellaneous
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
Yohimbine
  • Inhibits platelet aggregation
  • Acts as a stimulant
  • Desire enhanced
  • Positive effects on erection and ejaculation
  • Synthetic and herbal forms
  • Avoid with panic/ anxiety
  • Sexual obsessions and compulsions
  • Sexual phobias
  • Combination formulations –Zumba
ed medications
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
Medical Conditions
  • MS
  • Tumors-hypothalamic, frontal cortex, temporal lobes, septal nuclei, etc.
  • TBI
  • Nero syphilis
  • Mania
  • Kleine Levine-Sleeping Beauty Syndrome
  • Fetal alcohol and PDD
  • Epilepsy
summary
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
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