Lecture № 9

Drugs effecting function of Uterus

Abdullaev Dzhumadil, pharmD

-1-
Hypothalamus regulates pituitary's function

Posterior pituitary

-2-
The alpha subunits of these four human glycoprotein hormones are identical; however,
their beta chains are unique and confer biological specificity.

thyroid gland
-3- Free thyroxine (fT4)
 Inside the ovary are hundreds of thousands of follicles.
From first day of menstrual cycle a few follicles begin to
grow at the same time but stop growing around day 7 except
the one.

In a normal menstrual cycle one dominant follicle will grow

containing one egg. The follicle will get bigger until it ruptures at
ovulation which then releases the egg. This is usually around 14
days after the beginning of woman menstrual cycle.

-4-
 The endometrium is the inner epithelial
layer, along with its mucous membrane, of
the mammalian uterus. It has a basal layer
and a functional layer; the functional layer
Around day 12 the follicle secrets a large thickens and then is shed during
amount of estrogen into the bloodstream. menstruation in humans and some other
mammals, including apes

Estradiol Progesteron

FSH fimbriae
LH
Progesterone converts the endometrium to its
secretory stage to prepare the uterus for
implantation. During implantation and gestation,
progesterone appears to decrease the maternal 
immune response to allow for the acceptance of th
sections as stickers
pregnancy
-5-
 From 150 million
sermatozoids, several thousand
only reach the place of
fertilization to fertilize the
Sperm 2-5 ml >150 mln
single egg, the rest of them die

during sex, a man throws from 2 to 5 ml sperm into the vagina -6-
The placenta is a temporary fetal organ that begins developing
from the blastocyst shortly after implantation.

-7-
 Drugs effecting function of Uterus

Tocolytics
Drugs, strengthening of uterus Drugs, weakening uterus contractions.
rhythmic contractions.
Posterior pituitary hormones
Oxytocin, desaminooxytocin. β2-adrenomimetics
Partusisten (fenoterol)
Ergot alkaloids
Ergometrine,
Methilercometrine.  Antidysrhythmic
Magnesium sulfate MgSO4
Prostaglandins
PGE 2, PGF 2α
Misoprostol.

-8-
 Oxytocin is a nonapeptide hormone that has a central role in the
regulation of parturition and lactation. There is oxytocin receptor
(OTR) signaling and its role in the myometrium during pregnancy and
in labor.

Oxytocin works by increasing the

concentration of calcium inside
muscle cells that control
contraction of the uterus.
Increased calcium increases
contraction of the uterus.

-9-
 Posterior pituitary hormones
N Name Enteral Parenteral doses Half-life
doses
1 •Oxytocin 1mg 10 units/mL 1–6 min

Postpartum Hemorrhage
10 unit IM after delivery of placenta
Add 10-40 units; not to exceed 40 units; to 1000 mL of nonhydrating
IV solution and infuse at necessary rate to control uterine atony
Labor Induction
0.5-1 mUnit/min IV, titrate 1-2 mUnit/min q15-60min until
contraction pattern reached that is similiar to normal labor (usually 6
mUnits/min); may decrease dose after desired frequency of
contraction reached and labor has progressed to 5-6 cm dilation
Incomplete or Inevitable Abortion
10-20 mUnit/min; not to exceed 30 units/12 hr

- 10 -
Common side effects of oxytocin include:
• Slow heart rate
• Fast heart rate
• Premature ventricular complexes and other irregular heartbeats (arrhythmias)
• Permanent central nervous system (CNS) or brain damage, and death secondary to
suffocation
• Neonatal seizure
• Neonatal yellowing of skin or eyes (jaundice)
• Fetal death
• Low Apgar score (5 minute)
• Uteroplacental hypoperfusion and variable deceleration of fetal heart rate
• Inadequate fetal oxygen levels (hypoxia)
• Perinatal hepatic necrosis
• Fetal hypercapnia
• Severe decreases in maternal systolic and diastolic blood pressure, increases in heart
rate, systemic venous return and cardiac output, and arrhythmia

- 11 -
 Posterior pituitary hormones
N Name Enteral doses Parenteral Half-life
doses
2 •Desaminooxytocin 150 IU subglossal
It is not inactivated by 5h
oxytocinase and is 50–100
times more effective
than oxytocin. The recommended dosage for desaminooxytocin is 25 to 50
units buccal tablet every 30 minutes or as necessary.
Side effects
In therapeutic doses, demoxitocin does not cause clinically significant side effects. the use of
demoxytocin in high doses and increased sensitivity of the uterus can lead to the following side effects:
in the mother: uterine cramps (also when used in low doses), uterine hypertonicity, tetanic
contractions, uterine hyperactivity with uterine and vaginal tissue ruptures; nausea, vomiting,
hypersalivation, increased blood pressure, tachycardia, arrhythmia; death is possible. There is a risk of
disseminated intravascular coagulation (DVK);
in the fetus: bradycardia, arrhythmia, asphyxia, acute fetal hypoxia, staining of amniotic fluid with
meconium; death is possible;
in newborns: there may be jaundice, retinal hemorrhage.
- 12 -
 Ergot alkaloids

Mechanism of action
Ergot alkaloids have structures similar to the biogenic amines norepinephrine,
serotonin and dopamine. Vasoconstriction is produced by an agonist activity and
this effect varies with different vascular beds. Hyperthermia and uterine
stimulation are other effects.

Uses of Ergometrine
Ergometrine is used in the prevention of:
• Postpartum Hemorrhage While it acts at alpha-adrenergic, dopaminergic,
and serotonin receptors , it exerts on the uterus (and other smooth muscles).

- 13 -
 Ergot alkaloids
N Name Enteral Parenteral doses Half-life
doses
3 •Ergometrine  0.2 Mg Oral 0.2 Mg/ml 30-120 min.
Tablet

4 0,2 mg/ml), for IM 30–120 min

•Methilercometrine.  injection

Side effects:
• nausea, vomiting, stomach pain,
diarrhea, leg cramps, increased
sweating, skin rash, headache,
- 14 -
 Prostaglandins

Prostaglandin E2 (PGE2), also known as dinoprostone, is a naturally

occurring prostaglandin with oxytocic properties that is used as a
medication. Dinoprostone is used in labor induction, bleeding after
delivery, termination of pregnancy, and in newborn babies to keep the 
ductus arteriosus open
Mechanism of action
Dinoprostone-induced uterine contractions are
similar to those produced by the body during
spontaneous labor. Increases in the amplitude and
frequency of uterine contractions reduces cervical
tone, which produces cervical dilation.
- 15 -
 Prostaglandins
N Name Enteral doses Parenteral doses Half-life

10mg
5 •Dinoprostone vaginal insert 2.5 to 5 min
(PGE 2)
6 •Carboprost 0.5mg/3g
PGF 2α endocervical gel 250 mcg 1 mL IM 2.5 to 5 min

Prostaglandin F2α (PGF2α in prostanoid nomenclature), pharmaceutically
termed carboprost is a naturally occurring prostaglandin used in medicine to induce
labor and as an abortifacient

- 16 -
 Drugs, strengthening of uterus rhythmic contractions.
N Name Enteral Parenteral doses Half-life
doses
tablet 20–40 min.
•Misoprostol  100mcg
7 200mcg

Induction
2 of Labor  Side effects including:
25 mcg (1/4 of 100-mcg oral tablet) intravaginally initially, then repeat at • severe ongoing stomach
intervals not to exceed q3-6hr discomfort or diarrhea,
Not to be used in patients with previous cesarean delivery or major uterine • feeling very thirsty or
surgery hot,
Postpartum Hemorrhage • unable to urinate,
Prophylaxis: 600 mcg PO within 1 minute of delivery • heavy sweating, and
Treatment: 800 mcg PO once; use caution if prophylactic dose already given • hot and dry skin
and adverse effects present or observed
Treatment of Incomplete Abortion
600 mcg buccally once - 17 -
 Tocolytics
Drugs, weakening uterus contractions.
Partusisten (fenoterol)
Important indication for b2-adrenoceptor agonists is tocolysis with the
aim to reduce premature labor and fetal mortality. b2-Adrenoceptors
are dominant (80–85% b2- vs. 15–20% b1-adrenoceptors in pregnant
women) in the uterus, especially in the progesterone-dominant uterus.
They mediate muscle relaxation. In addition, there appears to be a
positive correlation between myometrial and b-adrenoceptor density
in the lymphocytes of pregnant women

- 18 -
 Drugs, weakening uterus contractions.
N Name Enteral Parenteral doses Half-life
doses
8 Partusisten 1 5 mg tablet 5 min
(fenoterol)
40mg/mL 5.2 h
Magnesium sulfate 80mg/mL
50%
9
MgSO4 Magnesium sulfate (MgSO4) can act as a
smooth muscle relaxant, possibly by blocking
calcium-mediated contraction, decreasing
acetylcholine release from neuromuscular
With doses of 20 and 40 micrograms Fenoterol, submaximal
junctions, and reducing histamine-induced
uterine relaxation times of 7.3 and 7.9 min were obtained.
airway spasm.
Subjective side effects such as palpitations and restlessness. 

- 19 -
 A
Bishkek city
Manas street 10

Rp: Misoprostol  800 mcg in tab.

D.t.d № 10
Sig: PO1 tab. a day
05.04.2021

- 20 -
 A
Bishkek city
Manas street 6

You should be able to

Rp: Magnesium sulfate
write a prescription
50%-10 mL in amp.
with each drugs
D.t.d № 5
Sig: 10 ml IV infusion in
5% dextrose 1 time a day
05.04.2021
- 21 -
 Thank you for your attention!

Abdullaev Dzhumadil, pharmD

- 22 -