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ANDRADE, Ma. Triza D.3E-Pharmacy

Pharmaceutical Chemistry II

+SEX HORMONES – Ovarian Hormones

NATURAL ESTROGENIC HORMONES AND DERIVATIVE

Estradiol Conjugated Estrogen Estrone Ethinyl estradiol

+Ethinyl Estradiol Estrogen, Ethinyl, Ethinylestradiol, Synthetic estrogen,

Estrogen in the pill, Mestranol, EE, Envoid A semisynthetic alkylated estradiol with a 17-alpha-ethinyl

substitution. is a synthetic form of estrogen and is mainly used in various

hormonal contraceptives -- usually in combination with a progestin.

It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives.

Marketed mostly in combination with othercompounds.

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tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2(7),3,5-triene-5,14-diol, (1S,10R,11S,14R,15S)-14-ethynyl-15-methyl-,

+tetracyclo[8.7.0.0²,7.0¹¹,¹⁵] heptadeca-2(7),3,5-triene-5,14-diol,

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+tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2(7),3,5-triene-5,14-diol, (1S,10R,11S,14R,15S)-14-ethynyl-15-methyl-,

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+STRUCTURE

+Mechanism of Action

Diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.

+EE is prepared from estrone in one step by ethinylation with ethyne, sodium and sodium amide

+INDICATION:

Moderate to severe vasomotor symptoms associated with the menopause

Female hypogonadism Prostatic carcinoma in the palliative therapy of

advanced disease Breast cancer Oral contraceptive Emergency contraceptive

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The lower ethinyl estradiol amounts now available in hormonal contraception enable women to obtain both the contraceptive and non-contraceptive benefits of birth control without as many of the unpleasant side effects. Ethinyl estradiol can assist in regulating your period or help manage painful periods. Because it helps to suppress ovulation, this synthetic estrogen has also been found to lower your risk of ovarian cancer, and due to estrogen’s ability to block bone resorption, ethinyl estradiol may help to increase bone mineral density.

+CONTRAINDICATION should not be used in women over 35 years old who smoke due to

the increased risk of serious cardiovascular side effects. Known or suspected carcinoma of the breast, except in selected

patients being treated for metastatic disease. Known or suspected estrogen dependent neoplasia. Known or suspected pregnancy. Active thrombophlebitis or thromboembolic disease. Undiagnosed abnormal genital bleeding. A past history of thrombophlebitis, thrombosis or thromboembolic

disease associated with the previous use of estrogen containing compounds.

+ADVERSE EFFECT

Water and sodium retention, which may result in edema, Weight gain, breast tenderness, and breast enlargement. Changes in libido and withdrawal vaginal bleeding are also reported.

Liver function impairment, jaundice and gallstones may occur. Headache, depression, dizziness, glucose intolerance, and sensitivity to

contact lenses are described. Large doses may produce hypercalcemia when used in the treatment of

metastatic carcinoma. Nausea, vomiting and diarrhea are not uncommon. Dermatological effects include chloasma, melasma, rashes and urticaria. Erythema multiforme and erythema nodosum occur. Hypertension and thromboembolic disease are reported.

+Brand Names

+ANTIDEPRESSANTS – Tricylic depressants Dibenzocycloheptadiene

Amitryptylline

+AMITRYPTILINE HYDROCHLORIDE dibenzocycloheptene-derivative tricyclic antidepressant

(TCA). . In non-depressed individuals, amitriptyline does not

affect mood or arousal, but may cause sedation. In depressed individuals, amitriptyline exerts a positive

effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake.

Tertiary amine TCAs, such as amitriptyline, are more potent inhibitors of serotonin

+Dimethyl amine, {3-[(2Z)-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene]propyl}-, Hydrochloride

+Dimethyl amine

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+Dimethyl amine, {3-[(2Z)-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene]propyl}-,

+

+Dimethyl amine, {3-[(2Z)-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene]propyl}-,

+

+Dimethyl amine, {3-[(2Z)-tricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene]propyl}-, Hydrochloride

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+Mechanism of Action

inhibition of neurotransmitter uptake (neuronal uptake of norepinerphrine and serotonin into presynaptic nerve terminals).

+INDICATION In the pharmacologic management of depressive illness may be used in the depressed phase of bipolar affective

disorder or in melancholic or psychotic depression. widely used as an atypical analgesic in the

management of several conditions including fibromyalgia and various neuropathies

 Amitriptyline can be also used in anxiety disorders, back pain, chronic fatigue syndrome, headache in adults and children, herpes zoster, Irritable bowel syndrome and pain control in palliative care

+Typical patient who may take Amitriptyline patient suffering from a Major Depressive Episode Depressed mood and/or loss of interest or pleasure

(irritability) Or any one of these:

+ANTINEOPLASTIC AGENTS – Alkylating agentsETHYLAMINES

Thiotepa

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