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DRUG TODAY-1

Presentation · July 2021

DOI: 10.13140/RG.2.2.14160.23045

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Magnesium sulfate
Group Antidysrhythmics, V; Electrolytes
[Magnesium sulfate is a drug used to treat convulsions during pregnancy,
nephritis in children, magnesium deficiency, and tetany.]
Generic Name Magnesium sulfate (Epsom salt)
Dosage • Injectable solution: 40mg/mL; 80mg/mL
• Infusion Solution: 1g/100mL: 2g/100mL
• Acute Nephritis: 100 mg/kg IM q4-6hr PRN or 20-40 mg/kg IM PRN
• Hypomagnesemia:
Adult:
Mild: 1 g intramuscularly (IM) every 6 hours for 4 doses
Severe: 5 g intravenously (IV) over 3 hours
Maintenance: 30-60 mg/kg/day IV
Paediatric:
Intravenous/intramuscular (IV/IM): 25-50 mg/kg every 4-6 hours for 3-4
doses as needed
Oral: 100-200 mg/kg every 6 hours
• Bronchospasm: 25-50 mg/kg IV over 10-20 minutes
• Preterm Labor (Off-label):
Loading dose: 4-6 g IV over 20 minutes; maintenance: 2-4 g/hr IV for 12-
24 hours as tolerated after contractions cease
Mode of Action • Magnesium is the second most plentiful cation of the intracellular fluids.
It is essential for the activity of many enzyme systems and plays an
important role with regard to neurochemical transmission and muscular
excitability.
• Magnesium sulfate reduces striated muscle contractions and blocks
peripheral neuromuscular transmission by reducing acetylcholine release
at the myoneural junction.
• Additionally, Magnesium inhibits Ca2+ influx through dihydropyridine-
sensitive, voltage-dependent channels. This accounts for much of its
relaxant action on vascular smooth muscle.
Route Oral and Parenteral
Indications • Used for immediate control of life-threatening convulsions in the
treatment of severe toxemias (pre-eclampsia and eclampsia) of pregnancy
and in the treatment of acute nephritis in children.
• Also indicated for replacement therapy in magnesium deficiency,
especially in acute hypomagnesemia accompanied by signs of tetany
similar to those of hypocalcemia.
• Also used in uterine tetany as a myometriat relaxant.
• Constipation (Oral magnesium sulfate is believed to help with
constipation by increasing water in the intestines.)
• Barium Poisoning
• Cerebral Edema
• Magnesium sulfate topical is used in the treatment of: Muscle Pain and
Muscle Spasm.
Contra Indication Magnesium sulfate has no known severe interactions with other drugs. But
serious interactions of magnesium sulfate include:
demeclocycline
doxycycline
lymecycline
minocycline
oxytetracycline

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

tetracycline
Side Effects Circulatory collapse
Respiratory paralysis
Low core body temperature (hypothermia)
Excess fluid in the lungs (pulmonary edema)
Depressed/poor reflexes
Low blood pressure (hypotension)
Flushing
Drowsiness
Depressed cardiac function/heart disturbances
Increased sweating
Low blood calcium (hypocalcemia)
Low blood phosphates (hypophosphatemia)
Low blood potassium (hyperkalemia)
Visual changes
Breathing difficulties
Confusion
Weakness
Flushing (warmth, redness, or tingly feeling)
Feeling like you might pass out
Anxiety
Cold feeling
Extreme drowsiness
Muscle tightness or contraction
Headache
Structure

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Oxytocin
Group Hormone & a Neurotransmitter
Generic Name Oxytocin (Love hormone)
Dosage • Injectable Solution: 10 units/mL
• Postpartum Haemorrhage:
- 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 similar 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.
Mode of Action - Oxytocin plays a vital role in labour and delivery.
- The hormone is produced in the hypothalamus and is secreted from the
paraventricular nucleus to the posterior pituitary where it is stored. It is
then released in pulses during childbirth to induce uterine contractions.
- The concentration of oxytocin receptors on the myometrium increases
significantly during pregnancy and reaches a peak in early labor.
- Activation of oxytocin receptors on the myometrium triggers a
downstream cascade that leads to increased intracellular calcium in
uterine myofibrils which strengthens and increases the frequency of
uterine contractions.
Route • IV infusion and IM injection
• Oxytocin may be administered either as an injection or a nasal spray.
because a nasal spray allows oxytocin to travel more readily from the
bloodstream to the brain than an injection.
Indications • Administration of exogenous oxytocin is indicated in the antepartum
period to initiate or improve uterine contractions for vaginal delivery in
situations where there is fetal or maternal concern.
• For example, it may be used to induce labor in cases of Rh sensitization,
maternal diabetes, preeclampsia at or near term, and when delivery is
indicated due to prematurely ruptured membranes.
• Oxytocin may be used to reinforce labor in select cases of uterine inertia
and as adjunctive therapy in the management of incomplete or inevitable
abortion.
• In the postpartum period, oxytocin may be used to induced contractions
in the 3rd stage of labor and to control postpartum bleeding or
haemorrhage.
• Oxytocin also serves a role in metabolic homeostasis and cardiovascular
regulation.
Contra Indication • Oxytocin injection is contraindicated in any of the following conditions:
- Significant cephalopelvic disproportion;
- Unfavourable fetal positions or presentations which are undeliverable
without conversion prior to delivery, i.e., transverse lies;
- In obstetrical emergencies where the benefit-to-risk ratio for either the
fetus or the mother favors surgical intervention;
- In cases of fetal distress where delivery is not imminent;
- Prolonged use in uterine inertia or severe toxemia;
- Hypertonic uterine patterns;

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

- Patients with hypersensitivity to the drug;

- Induction or augmentation of labor in those cases where vaginal delivery
is contraindicated, such as cord presentation or prolapse, total placenta
previa, and vasa previa.
Side Effects • Administration of supratherapeutic doses of exogenous oxytocin can lead
to myocardial ischemia, tachycardia, and arrhythmias.
• High doses can also lead to uterine spasms, hypertonicity, or rupture.
• Oxytocin has antidiuretic properties, thus, high daily doses (as a single
dose or administered slowly over 24 hours) may lead to extreme water
intoxication resulting in maternal seizures, coma, and even death.
• Uteroplacental hypoperfusion and variable deceleration of fetal heart rate.
• Perinatal hepatic necrosis.
• Inadequate fetal oxygen levels (hypoxia).
Structure

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Methylergometrine or Methylergonovine
Group Post-delivery bleeding
Generic Name Methylergometrine
Trade Name Methergine
Dosage • Intramuscularly
- 1 mL, 0.2 mg, after delivery of the anterior shoulder, after delivery of
the placenta, or during the puerperium. May be repeated as required,
at intervals of 2-4 hours.
• Intravenously
- 1 mL, 0.2 mg, administered slowly over a period of no less than 60
seconds.
• Orally
- One tablet, 0.2 mg, 3 or 4 times daily in the puerperium for a
maximum of 1 week.
Mode of Action - This medication is used after childbirth to help stop bleeding from the
uterus.
- Methylergonovine belongs to a class of drugs known as ergot alkaloids.
- It works by increasing the rate and strength of contractions and the
stiffness of the uterus muscles. These effects help to decrease bleeding.
- Methylergometrine acts directly on the smooth muscle of the uterus and
increases the tone, rate, and amplitude of rhythmic contractions through
binding and the resultant antagonism of the dopamine D1 receptor.
- Thus, it induces a rapid and sustained tetanic uterotonic effect which
shortens the third stage of labor and reduces blood loss.
Route Oral and Parenteral
Indications • For the prevention and control of excessive bleeding following vaginal
childbirth.
Contra Indication • Methylergometrine likely interacts with drugs that inhibit the liver
enzyme CYP3A4, such as azole antifungals, macrolide antibiotics and
many HIV drugs.
• It can also increase constriction of blood vessels caused by
sympathomimetic drugs and other ergot alkaloids.
Side Effects - Nausea, vomiting, and diarrhoea
- Dizziness
- Pulmonary hypertension
- Coronary artery vasoconstriction
- Severe systemic hypertension (especially in patients with pre-eclampsia)
- Convulsions
- In excessive doses, methylergometrine can also lead to cramping,
respiratory depression and coma.
Structure

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Pethidine
Group Opioid Agonist
Generic Name Meperidine or Pethidine
Trade Name Demerol
Dosage • Syrup: 50mg/5mL
• Tablet: 50 mg; 100 mg
• Injectable Solution: 25mg/mL; 50mg/mL; 75mg/mL; 100mg/mL
• Meperidine/ Pethidine is not recommended as a first-choice analgesic by The
American Pain Society.
- Pain: 50-150 mg PO/IM/SC q3-4hr PRN; adjust dose-based degree of
response
- Preoperatively: 50-100 mg IM/SC 30-90 min before beginning anaesthesia.
- Continuous infusion: 15-35 mg/hr
- Obstetrical analgesia: 50-100 mg IM/SC; repeated q1-3hr PRN
[PRN (pro re nata): "when necessary"]
Mode of Action - Pethidine exerts its analgesic effects by acting as an agonist at the μ-opioid
receptor.
- Pethidine is often employed in the treatment of postanaesthetic shivering. The
pharmacologic mechanism of this antishivering effect is not fully understood,
but it may involve the stimulation of κ-opioid receptors.
- In addition to these opioidergic and anticholinergic effects, it has local
anaesthetic activity related to its interactions with sodium ion channels.
Route Oral & Parenteral
(Pethidine is mostly administered intravenously, intramuscularly or
intrathecally.)
Indications • Used to control moderate to severe pain.
• Pethidine can be used for preoperative management of musculoskeletal and
visceral pain, for premedication before general anaesthesia, as an adjunct to
inhalational and other anaesthetic agents, to prevent tachypnea (abnormally
rapid breathing) induced by trichloroethylene (an inhaled anaesthetic), alone
or in combination with diazepam for pain reduction in fractures and other
minor interventions, for postoperative analgesia or for obstetric analgesia.
• It is commonly used for pain relief during labor and delivery.
Contra Indication - Pethidine has serious interactions that can be dangerous with monoamine
oxidase inhibitors (e.g., furazolidone, isocarboxazid, moclobemide,
phenelzine, procarbazine, selegiline, tranylcypromine).
- It can interact as well with SSRIs (Selective serotonin reuptake inhibitor) and
other antidepressants, antiparkinson agents.
- It also interacts with a number of other medications, including muscle
relaxants, benzodiazepines, and ethanol.
Side Effects - Dependence, confusion, mood altered, mild euphoria, hallucinations,
dysphoria, agitation, anxiety, nervousness. Increased risk of delirium in
elderly patients.
- The most serious adverse effects of pethidine are respiratory depression and
hypotension.
Structure

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Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Misoprostol
Group Prostaglandin E1 analogue
Generic Name Misoprostol
Trade Name Arthrotec, Cytotec, Mifegymiso
Dosage • NSAID-Induced Ulcer
✓ Adult
- Prophylaxis: 200 mcg orally every 6 hours with food; may be decreased to
100 mcg every 6 hours if higher dose is not tolerated; last dose to be
administered at bedtime.
- Geriatric: To avoid possibility of diarrhoea, dosing may be initiated at 100
mcg every 6 hours and increased by 100 mcg/day every 3 days until desired
dose is achieved.
• Stress Ulcer Prophylaxis (off-label): 100-200 mcg orally every 4-6 hours.
• Induction of Labor (off-label): 25 mcg (1/4 of 100 mcg oral tablet)
intravaginally initially, then repeat at intervals not to exceed every 3-6 hours.
• Postpartum Hemorrhage (off-label):
- Prophylaxis: 600 mcg orally within 1 minute of delivery
- Treatment: 800 mcg orally once; use caution if prophylactic dose already
given and adverse effects present or observed
- Use only in settings were oxytocin not available.
• Pediatrics
- Children under 8 years: Safety and efficacy not established
- Children 8 years and older: 100 mcg orally every 6 hours.
Mode of Action - Misoprostol is a synthetic prostaglandin E1 analog that stimulates
prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric
acid secretion.
- Misoprostol binds to smooth muscle cells in the uterine lining to increase the
strength and frequency of contractions as well as degrade collagen and reduce
cervical tone.
Route - Sublingual; oral and vaginal.
Indications - Misoprostol is a prostaglandin analog used to reduce the risk of NSAID
related ulcers, manage miscarriages, prevent post-partum hemorrhage, and
also for first trimester abortions.
- Misoprostol is commonly used for labor induction. It causes uterine
contractions and the ripening (effacement or thinning) of the cervix.
- Misoprostol is used either alone or in conjunction with another medication
(mifepristone or methotrexate) for medical abortions as an alternative to
surgical abortion.
- Misoprostol may be used to complete a miscarriage or missed abortion when
the body does not expel the embryo or fetus on its own.
- In women with prior caesarean section or prior failure of insertion of an
intrauterine contraceptive device, pre-procedure administration of
misoprostol reduces the rate of failure of insertion of intrauterine
contraceptive device.
Contra Indication Medical treatment for a missed abortion with misoprostol should only be
considered in people who do not have any of the following contraindications:
suspected ectopic pregnancy, nonsteroidal drug use, signs of pelvic infections
or sepsis, unstable hemodynamics, known misoprostol allergy, previous
caesarean section, mitral stenosis, hypertension, glaucoma, or bronchial
asthma.

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 Dr. Sumanta Mondal_Lecture Notes_GITAM (Deemed to be University) DRUG TODAY-1

Side Effects - Common side effects: abdominal pain, nausea, flatulence, headache,
dyspepsia, vomiting, and constipation.
- Note By: Misoprostol should not be taken by pregnant women with wanted
pregnancies to reduce the risk of NSAID-induced gastric ulcers because it
increases uterine tone and contractions in pregnancy, which may cause partial
or complete abortions, and because its use in pregnancy has been associated
with birth defects.
- There are increased side effects with sublingual or oral misoprostol,
compared to a low dose (400 ug) vaginal misoprostol. However, low dose
vaginal misoprostol was linked with low complete abortion rate.
Structure

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