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Sexual Pharmacology

This presentation explores the relationship between common medications and sexuality, including hypersexuality. It discusses relevant brain structures, chemistry, and processes involved in sexuality and addresses the ethical considerations related to this topic.

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Sexual Pharmacology

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  1. Sexual Pharmacology Susan J Campling, RN, Psy.D Director of Special Projects Pine Grove Behavioral Health Hattiesburg MS 39402

  2. 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

  3. 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

  4. 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

  5. HaroutunianImperative “Every addiction presentation must have at least one brain slide.”

  6. 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

  7. Brain Region of the Day The Insula!!!

  8. 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.

  9. 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

  10. Maternal love and romantic love are more alike than lust yet there is significant over- lap.

  11. IvankaSavic and Per Linstrom, Stockholm Brain Institute, April 2008, Pet and MRI Differences in cerebral asymmetry and functional conductivity between homo and heterosexual subjects

  12. Direct Side Effects Back to medications • Anorgasmia • Sex drive disorders • Dyspareunia • Anesthetic orgasm • Retrograde ejaculation • Priapism • Gynecomastia • Clitoral hypertrophy

  13. Direct Side Effects • Infertility/ sterility • Hormonal- gynecomastia, hypogonadism • Menstrual disorders What is priapism?

  14. Indirect Side Effects • Body image • Comfort • Odors/ taste alteration • Gastrointestinal side effects • Urinary tract • Neurological • Cardiovascular • Skin • Sensory impairment

  15. FYI • Agonist stimulate and facilitate a response in a pathway • Antagonist act against the pathway a

  16. 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

  17. 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 

  18. 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

  19. 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

  20. Excitatory • Testosterone • Zinc- needed for spermatogenesis: reduces GABA and endogenous opioids • Estrogens- essential to female desire, attraction, lubrication orgasm, satisfaction, • Histamine • Oxytocin/ vasopressin*

  21. 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

  22. 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

  23. 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?

  24. 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?

  25. 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)

  26. 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

  27. 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

  28. 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

  29. 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

  30. 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

  31. 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)

  32. 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?

  33. 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.

  34. 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

  35. 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

  36. 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

  37. 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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