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Aphrodisiacs agents by Kashikant Yadav

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Screening methods of Aphrodisiacs Agents

Published in: Health & Medicine
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Aphrodisiacs agents by Kashikant Yadav

  1. 1. SCREENING METHODS OF APHRODISIACS AGENTS BY : Kashikant Yadav M pham (Pharmacology) ykashikant@gmail.com
  2. 2. Contents:  Definition  Aphrodisiacs Drugs  Mechanism involved in Aphrodisiacs Drugs  Purposes of Aphrodisiacs Agents  Side Effects  Screening Methods of Aphrodisiac Agents
  3. 3. Aphrodisiacs Agents  drugs that arouse or increase sexual desire or excitement  substance that increases libido when consumed
  4. 4. Aphrodisiacs Drugs  Sildenafil citrate  Arginine  Testosterone  Crocin  Phenethylamines  Amphetamine  Methamphetamine
  5. 5. Mechanism involved in Aphrodisiacs Drugs  These drugs act by enhancing the sex organ sensation and performance. They improve the blood flow to the male sex organs, thus improving the male libido. A similar response in women may also produce an increased sexual stimulation.  One of the mechanisms by which cyclic nucleotides induce the relaxation of smooth muscle is through the opening of potassium (K+) channels, which leads to the efflux of K+ from the smooth muscle cell, down their electrochemical gradient. This results in hyperpolarization and an inhibitory effect on trans membrane Ca2+ flux and eventually, smooth muscle relaxation.
  6. 6.  Another mechanism which causes penile erection is through cyclic adenosine monophosphate pathway (cAMP). Corporal smooth muscle relaxation is mediated via cAMP. The activated membrane-bound adenylyl cyclase, which generates cAMP, it activates protein kinase A and to a lesser extent, protein kinase G. Prostagladin E1 also increases the intracellular concentrations of cAMP in the corpus cavernosum smooth muscle cells. The generation of cAMP activates the Ca2+ pump and consequently, the level of free cytoplasmic Ca2+ is reduced, resulting in smooth muscle relaxation. Similarly, the protein kinase activates the cell- membrane Ca2+ pump, leading to a decreased sarcoplasmic Ca2+ concentration which induces a loss of contractile tone of the penile smooth muscle and increase of blood flow in the cavernous body resulting in erection.
  7. 7. Purposes of Aphrodisiacs Agents To increase low libido. To improve sexual performance. In the treatment of impotence To treat physiological problems that affect sexual activity
  8. 8. Side Effects  arrhythmia of the heart  suicidal tendencies  mental disorders  tremors  headaches  fainting facial flushing  upset stomach  blurred vision  sensitivity to light usually occur with high doses.
  9. 9. Screening Methods of Aphrodisiac Agents A) Physical or behavioral methods ( In vivo Method) i) Mating behavior test ii) Libido test iii) Potency test iv) Orientation activity test v) Sexual and vital organ weight test B) Biochemical or Hormonal Methods ( In vitro Method) i) Estimation of cholesterol level ii) Estimation of sex hormones level iii) Assay for nitric oxide synthase iv) Assay for androgen receptor protein
  10. 10. Physical or behavioral methods i) Mating behavior test  Healthy and sexually experienced male rats (200-300 gm) with brick sexual activity are divided into three groups (n=6)  Group-I , receives distilled water(10ml/kg, p.o.)  Group-II, receives testing agent daily for 21 days  Group-III, receives standard drug i.e. sildenafil (5mg/kg, p.o.) one hour prior to the experimentation  Than all the animals are exposed to dim light (1 w fluorescent tube in a laboratory of 14’ x14’) at the stipulated time of testing daily for 6 days prior the test
  11. 11.  Female rates treated with ethinyl estradioal (100μg/animal p.o.) 48hrs and with progesterone (1mg/animal, s.c.) 6hrs before pairing (1:1 ratio)  On 21st day , the experiment is conducted at 8pm and the male rats are observed for-  Mounting frequency  Intromission frequency  Mounting latency  Intromission latency  Ejaculation latency  Post-ejaculation interval  Libido index  Compute above parameters of male sexual behavior and compare between testing agent , control and standard drug.
  12. 12. ii) Libido test  Healthy and sexually experienced male rats (200-300 gm) with brick sexual activity are divided into three groups (n=6)  Group-I , receives distilled water(10ml/kg, p.o.)  Group-II, receives testing agent daily for 21 days  Group-III, receives standard drug i.e. sildenafil (5mg/kg, p.o.) one hour prior to the experimentation  Than all the animals are exposed to dim light (1 w fluorescent tube in a laboratory of 14’ x14’) at the stipulated time of testing daily for 6 days prior the test
  13. 13.  The female rats should be made to receptive by hormonal treatment  On the evening of 21st day the penis should be exposed by retracting the sheath and applying xylocaine 5 % ointment, 30,15 and 5 min before the observation for mating frequency, intromission and ejaculation .  Compare the data between testing agent , vehicle control and standard drug treated groups.
  14. 14. iii) Potency test  Healthy and sexually experienced male rats (200- 300 gm) with brick sexual activity are divided into three groups (n=6)  Group-I , receives distilled water(10ml/kg, p.o.)  Group-II, receives testing agent daily for 21 days  Group-III, receives standard drug i.e. sildenafil (5mg/kg, p.o.) one hour prior to the experimentation
  15. 15.  On 21st day, the rat is placed on back with partial restraint  The preputial sheath is pushed behind the glans by thumb and index figure and rat is holded in this manner for 15 min then the total penile relaxes is recorded  Compare the data between testing agents, vehicle and standard drug treated groups.
  16. 16. Biochemical or Hormonal Methods a) Estimation of sex hormones level  Testing agent which produce significant reduction of prolactin in males should enhance the levels of luteinizing hormones, follicle stimulating hormones and testosterone  The estimation of serum concentration of above hormones leads to evaluation of aphrodisiac agents
  17. 17. ii) Assay for nitric oxide synthase  NO relaxes the smooth muscles of cavernosum which leads to increase in flow of blood into male sex organ  Therefore, estimation of NOs in male copulatory organ and testes of treated and control groups help to evaluate aphrodisiac activity of testing agents.

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