Testosterone is converted to dihydrotestosterone (DHT) by the enzyme 5-alpha reductase.

5-alpha reductase

يا نوع من العلاجات الي اخذناهن باقي المحاضرات
يكون الطرح مالتهن عن طريق feces

يا علاج يقلل نسبة LDL

ويا علاج يزيد نسبة LDL

الي يزود صح هو testosterone

لكن الي يقلل هو الاستروجين و بالضبط raloxifene

عدنا الانتي اندروجين اكو نهايتهم mide يكون عملهن تنافسي ع نفس الرسبتور مال testosterone
اي تعتبر antagonist استخدمهم بحالة ال prostate cancer



والي نهايتهم ride يكون عملها تثبيط للانزايم الي اسمه
5-alpha reductase
الي يحول testosterone الى مركبه النشط
يعني راح يقلل من تكوين DHT و بالتالي قللت تأثير testosterone
يستخدم لل prostate hyperpy

#contraceptive

ملاحظات محاضرة contraceptive ☝🏻💯

🔔طلاب الفارما

🈂يلا نراجع كل الادوية المذكورة بلكجر 8️⃣

Lec 8️⃣ I Estrogen and androgen

🕊️Estrogens

💊Estradiol ➡️ most potent estrogen produced and secreted by ovary

💊Estrone ➡️ is a metabolite of estradiol and is primary circulating estrogen after menopause

💊Estriol ➡️ another metabolite of estradiol and it is less potent than estradiol

🕊️Synthetic estrogen

💊Ethinyl estradiol
💊Estradiol valerate ➡️ prodrug of estradiol

3️⃣Selective estrogen receptor modulator

💊Tamoxifen
💊Raloxifen
💊Bazedoxifen
💊Clomiphene
💊Ospemifene

4️⃣Progesterones

💊Desogestrel
💊Dienogest
💊Levonorgestrel
💊Norethindrone
💊Norethindrone acetate
💊Norgestimate
💊Norgestrel
💊Medroxyprogestrone acetate

5️⃣Progestine have androgenic activity

💊Norethindrone acetate
💊Norethindrone
💊Norgestrel
💊Levonogetrel

6️⃣less androgenic progestin

💊Norgestimate
💊Drosperinone

🔴Antiprogestin

💊Mifepristone

#estrogen

#estrogen and androgen

ملاحظات كتبتها اثناء الشرح
Estrogen P2

#estrogen

ملخص لل SERM

⭕ Tamoxifen

At bone Agonist
يفيدنه في علاج الـ Osteoporosis

At breast Antagonist
يفيدنه في علاج breast cancer

At endometrium Agonist
ممكن يسبب endometrium cancer

⭕ Raloxifen

At bone Agonist
يفيدنه في علاج الـ Osteoporosis

At breast Antagonist
يفيدنه في علاج او الوقاية من breast cancer

At endometrium Antagonist
ما يسبب endometrium cancer عكس ال Tamoxifen


⭕ Bazedoxifene

At endometrium
يكون antagonist في ال endometrium
لذلك ممكن نضيفه وي ال Estrogen therapy في حالة النساء الي عدهم intact uterus ويعانن من اعراض انقطاع الطمث menopausal symptoms
حتى نقلل من ال risk of endometrium cancer الي يسببه ال Estrogen


⭕ Ospemifene

هذا الشي المميز بيه يستخدم في حالة dyspareunia الي هي الالم الي يصير بعد الجِماع
(painful sexual intercourse)

⭕ Clomiphene

هذا آلية عمله مميزة يكون Partial Estrogen Agonist
يتداخل وي ال negative feedback on hypothalamus
ويساهم في زيادة افراز ال FSH and LH
لذلك يستخدم في علاج العقم infertility

حتى ما تشبش عدكم التأثيرات والاستخدامات

#estrogen

اهم شي اضبط مادة مو اخلض

💡طلاب الفارما لاتنسون هذا الفرق بين ال

👉Raloxifen & Tamoxifen

💡Raloxifen is an estrogen antagonist in uterine and breast tissue❌❌
& agonist in bone ✅✅

يعني ال Raloxifen مايسبب ال
Endometrial cancer ✅✅


But

💡Tamoxifen is an estrogen antagonist in breast tissue ❌❌
&
agonist in bone and endometrium ✅

يعني ممكن يسبب ال
Endometrial cancer 🥲🥲
#estrogen

1.Ospemifene may
stimulate
endometrial growth,
and addition of a
progestogen in
2.women with an
intact uterus should
be considered.


Raloxifen
1.Hot flashes and leg
cramps are common
adverse effects
withraloxifene.
2.there is an increased
risk of deep vein
thrombosis and
3.pulmonary
embolism


Tamoxifen
• 1-Predicpose to
endometrial cancer
and hyperplasia
• 2- High rate of drug-
drug interaction



&&&

Clomiphine
citrate
• 1- Ovarian enlargement
• 2- Risk of multiple
pregnancy.
• 3- Visual disturbance
• 4- Hot flush and leg cr
s.e #estrogen

Prevention of Osteoporosis

💛To reduce bone loss in postmenopausal women include
حتى نحد من فقدان العظم عند النساء بعد انقطاع الطمث تتضمن التالي
1-intake of calcium and vitamin D
2-weight-bearing exercise
3-smoking cessation
3- avoidance of excessive alcohol intake

💛 Patients with inadequate dietary intake of calcium should receive calcium supplementation such as
المرضى لي يعانون من عدم كفاية تناول الكالسيوم في الجسم ننطيهم مكملات الكالسيوم مثل
1- Calcium carbonate
2-Calcium citrate

Adverse effects of calcium supplementation

💚 gas and bloating

💚Calcium may interfere with absorption of
-iron preparations
-thyroid replacement
-fluoroquinolone
-tetracycline antibiotics

and administration of these drugs should be separated by several hours.

Mechanisms

💚Bisphosphonates
1- bind to hydroxyapatite crystals in the bone and decrease osteoclastic bone resorption
2-resulting in a small increase in bone mass and a decreased risk of fractures in patients with osteoporosis
……………………………………………………….

💙Denosumab
1- monoclonal antibody that targets receptor activator of nuclear factor kappa-8 ligand
and inhibits osteoclast formation and function
……………………………………………………….

🩷Parathyroid agents (Teriparatide,abaloparatide)

1-act as agonists at the parathyroid hormone receptor
and once-daily subcutaneous administration results in stimulation of osteoblastic activity and increased bone formation and bone strength
……………………………………………………….
🩵Selective estrogen receptor
modulators(Raloxifene)

1- is a selective estrogen recentor modulator approved for the prevention and treatment of osteoporosis
……………………………………………………….
🧡Calcitonin(salmon calcitonin)
reduces bone resorption

#bone

Adverse effects

💊Bisphosphonates
1- diarrhoea
2-abdominal pain
3- musculoskeletal pain.
4-Alendronate, risedronate, and ibandronate —-> associated with esophagitis and esophageal ulcers
5- Bisphosphonates—-> osteonecrosis of the jaw and atypical femur fractures may occur and risk increase with long-term use of bisphosphonates.

💊Denosumab
1-increased risk of infections
2-dermatological reactions
3-hypocalcemia
4-rarely, osteonecrosis of the jaw
5-atypical fractures

💊Parathyroid agents
1-hypercalcemia
2-orthostatic hypotension
3-increased risk of osteosarcoma in rats

💊Selective estrogen receptor modulators

1-hot flashes
2-leg cramps
3-increased risk of venous thromboembolism

💊Calcitonin
1-rhinitis
2-nasal symptoms
#bone

دلائل مهمه لمعرفة نوع الفلتر
كل فلتر خليت الميزة المهمه والي عسى ولعل تجي بالامتحان .

Gravity filter➡️1)generated low pressure
2) common in water treatment
ومتوفر بشكل candles ,cylindrical , rectangular, hydro clear

Vacuum Filter :
A) Rotary Drum Filter ➡️
مراحل الoperation
1)Agitator 2)pick up zone-3)drying zone -4)cack removing zone

Precoat of filter aids used when very high degree of clarity required,or solid content is very low or sticky solid

B) Rotary Disc Filter ➡️ 1-have large surface area in less floor space , 2-the lowest cost Compared to other vacuum

Pressure filters :
A) plate and Frame filter press ➡️ Most verastile , can used for both coarse and fine filtration

B) Disc Filter ➡️ The flow may be from inside outward or outside inward

Centrifugation filtration :
effective washing and drying
ال moisture المتبقية تكون اقل بكثير من الي بالفلاتر السابقة وتصل الى اقل من 3%

#filtartion

دلائل لمعرفة نوع ال mixer
(فقط batch mixer)
Liquid mixing
Propeller➡️efficient When they are run at high speed in liquid with low viscosity

Turbines ➡️ can be operated satisfactorily in fluid 1000 times more viscous than fluid in propeller

Paddles➡️ 1)Their blades have large surface area as compared to the tank in which they are employed
2)they pass close to the tank walls and effectively mix viscous fluids and semisolid

Air jet➡️ يستخدم هواء او غاز
fluid should be 1)low viscosity 2)nonfoaming
3)non reactive with gse
4) non volatile

Fluid jet ➡️ fluid are pumped through nozzles

Semisold mixing
Sigma-blade mixer ➡️ the blade rotate tangentially in 2:1 speed ratioo. Effective in de aggregation as well as distribution of solid in fluid.

Planetary mixer ➡️ the mixing arm rotates around itself and around circumference of containar

Mulling mixer ➡️efficient in the de aggregation of solid , these devices suitable for mixing previously mixed material but contain aggregate.
فرقها عن ال sigma blade انو هي فعاله فقط ب de aggregation

Solid mixing

1)Tumbler➡️ Efficient not aggressive (good for friable powder)

من ضمن انواعه
V-shaped mixer(twin shell mixer) ➡️ consists of 2 cylinder connected at 45 angle
يصير بي convective و shear

2) agitator mixer ➡️ more effective in mixing wet powder that don’t mix well in tumbler, effective in breaking up lumps

من ضمن انواعه هو
Ribbon mixer ➡️ consist of horizontal cylindrical tank usually opening at top
#mixing