Ministry of higher education and scientific research

Middle technical university, college of health and medical

techniques, anesthesia techniques department, 2nd.Stage

Teaching package for basics of anesthesia 2

By Dr. Hussam Kareem Mghames

MBChB/F.I.C.M.S Anesthesia and Intensive care 2023-2024

(From 1 to 15 weeks)
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Drugs used in Premedication:

Anxiolytic drugs

These drugs used to decrease the anxiety of the patients and make him
sedative and calm with amnesia (unable to remember)

They act predominantly on GABA receptors

Minimum cardiac and respiratory depression

Do not produce nausea and vomiting

Lack the analgesic effect

Cross the placenta and may cause neonatal depression

The main drugs that used are the benzodiazepines;

diazepam, midazolam, lorazepam, alprazolam.

The benzodiazepines exhibit anxiolytic, sedative, amnesic and

anticonvulsant properties.

They differ mainly in their pharmacokinetic properties, some being relatively

short acting whereas others are only slowly eliminated. For many years
diazepam has been the dominant sedative and anxiolytic for oral
premedication. It is rapidly absorbed when given by mouth and in the
standard dose of 10 to 20 mg exerts an anxiolytic action similar to that of
morphine

Diazepam causes anterograde amnesia and is devoid of emetic side effects.

Its main disadvantages are a variable and unpredictable anxiolytic and
sedative action and a long elimination half-life. Its duration of action is
further prolonged by active metabolites. Intramuscular injection is painful and
is not recommended.

Midazolam is a water-soluble benzodiazepine, a member of a new class of

imidazobenzodiazepine derivative. It is water soluble at pH< 4 but becomes
highly lipid soluble at physiologic ph. Water solubility minimizes pain at the
injection site. The lipid solubility ensures rapid distribution in tissues.
Midazolam is more potent, has a faster onset and shorter duration of action
than diazepam. The elimination half-life is 1.5 to 3.5 hours as against
approximately 20 hours in case of diazepam. The metabolites of midazolam
have negligible soporific effects. These properties make midazolam a suitable
agent for producing conscious sedation in short endoscopic procedures, pre
operative sedation and for induction of general anesthesia., midazolam has
been found to provide pre-operative sedative effect superior to that of

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diazepam The drug has shown good local tolerability as well as good
hemodynamic stability.
Analgesic drugs

Analgesic drugs given pre-operatively reduce the required dose of anesthetic

agent and improve patient comfort in the immediate postoperative period.

Options used include opioids, paracetamol, non-steroidal anti-inflammatory

drugs (NSAIDs)

• NSAIDs are commonly used, particularly in day surgery, unless there

are contra-indications.
• Opioids are usually the agents of choice in the presence of acute

severe pain. In the absence of pain, some people may experience

intense dysphoria. Opioids also cause variable sedation and
cardiorespiratory depression. All opioids can cause nausea and
vomiting and this may outweigh any beneficial effects. Opioids may
also precipitate bronchospasm or anaphylaxis.
• Clonidine given as a premedication has been shown to reduce

postoperative pain in children

• Relevant pre-operative pain relief naturally depends on the nature of

the procedure as well as factors relating to the individual patient.

Classifications of opioids

➢ Natural Opium Alkaloids: Morphine and Codeine

➢ Semi-synthetic: Diacetylmorphine (Heroin) and Pholcodeine

➢ Synthetic Opioids:
Pethidine (Mepiridine) and its congeners Diphenoxylate and Loperamide
Fentanyl and its congeners fentanyl, and remifentanil

Can be given parentally

Produce sedation

Control elevated blood pressure during endotracheal

intubation Pethidine versus morphine

➢ 1/10th as potent as Morphine, but Efficacy is similar

➢ Produces as much sedation, euphoria and respiratory depression

in equianalgesic dose and similar abuse potential
➢ Less spasmodic action in smooth muscles

➢ less miosis, constipation and urinary retention

➢ Rapid but short duration of action (2-3 Hrs)

➢ Vagolytic effect

➢ Tachycardia – Devoid of antitussive action

➢ Less histamine releases

➢ safer in asthmatics

• Pharmacokinetics

➢ Well absorbed orally,

➢ bioavailability 50%

➢ Effects appear in 10-15 min. after oral absorption

➢ On parenteral administration action lasts for 2-3 Hrs

➢ Metabolized in liver, Excreted in urine

Fentanyl:

Potent analgesic 100 times more than morphine

Metabolized in the liver and excreted in the urine

Produce respiratory depression so use in caution with

COPD Cause less nausea and vomiting

Can be reversed by naloxone

Dose 1-5 microgram / kilogram i.v

Fentanyl is preferred due to its rapid onset and short duration of action

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Remifentanil

Remifentanil (marketed by Abbott as Ultiva) is a potent ultra-short-acting

synthetic opioid given to patients during surgery for pain relief and adjunctive
to an anesthetic. Remifentanil is a specific mu-type-opioid receptor agonist
which means it reduces sympathetic nervous system tone, and causes
respiratory depression and analgesia.

Remifentanil is an opioid agonist with rapid onset and peak effect and ultra
short duration of action. The opioid activity of remifentanil is antagonized by
opioid antagonists such as naloxone. The analgesic effects of remifentanil are
rapid in onset and offset. Its effects and side effects are dose dependent and
similar to other opioids. (Hypotension is the most common side effects)

Anti-autonomic drugs

and they contain either anticholinergic or beta1blocker

The anticholinergic drugs that used in the premedication are;

Atropine, hyoscine and Glycopyrrolate.

➢ Atropine has vagal inhibition (tachycardia), CNS

stimulation, Antisialagogues (decrease salivation). The dose of

atropine is 0.3 – 0.4 mg iv

Atropine may cause central anticholinergic syndrome (restlessness, agitation,

somnolence, convulsion) and this can be reversed by physostigmine

➢ Hyoscine had less vagal inhibition effect with more effect on

salivation but produce sedation and amnesia so should be avoided

in elderly

➢ Glycopyrrolate has no central action because it does not cross the blood
brain barrier, had longer duration and less tachycardia

They produce dry mouth

They produce mydriasis (dilation of eye pupil) except Glycopyrrolate

Antiemetic drugs

they are drugs used to decrease the incidence of nausea

and vomiting, the most commonly used are: ondansetron

and Metoclopramide (plasil)

The most common used antiemetic drug

Dose 0.15 to 0.3 mg /kg and last for 12 hours

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Used in emergency anesthesia
Act centrally as dopaminergic antagonist on the vomiting center in the
medulla

Act peripherally by increasing the rate of gastric emptying and

increasing in the gut peristalsis

May produce oculogyric (extrapyramidal) side effect

Ondansetron

Ondansetron is a selective 5-HT3 serotonin-receptor antagonist used for its

antiemetic properties.

Ondansetron acts both centrally and peripherally to prevent and treat nausea
and vomiting.

Central effects are mediated by the antagonism of 5HT-3 serotonin receptors.

Ondansetron also has effects peripherally by acting on the vagus nerve. It
works on the 5-HT3 receptors that can be found at the vagus nerve terminals.
The vagus nerve can sense nausea and vomiting triggers within the GI tract,
such as stomach irritants. The peripheral actions of ondansetron are thought
to be the predominant mechanism for its antiemetic effects.
Antacid drugs

these are drugs that used to increase the PH of the gastric

juice and decrease volume and so decrease the side effect of the

pulmonary aspiration if happen

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They are not recommended to the patient with no risk of aspiration
Histamine H2 receptors antagonists also known as H2-blockers (cimetidine
and ranitidine are the most commonly used) they act on the histamine
receptor and increase the ph. of the gastric content

proton pump inhibitors like Omeprazole, lansoprazole also used antiacid

drugs

The other drug was sodium citrate given 15 to 30 min before

anesthesia to also increase the ph. of the gastric content

The oral route is better than the iv in this type of drugs

MCQ TEST

1- All the following are true regarding Glycopyrrolate except one

a) Anticholinergic drug
b) Increase heart rate.
c) Causes sedation
d) Not pass placenta
e) No antiemetic effects
2- Fentanyl (all true except one)
a) Potent analgesic 100 times more than morphine
b) Metabolized in the liver and excreted in the urine
c) use in caution with COPD
d) Cause less nausea and vomiting
e) Can be reversed by neostigmine
3- Metoclopramide (all true except one)

a) The most common used antiemetic drug

b) Act centrally as dopaminergic antagonist on the vomiting
center in the medulla
c) Act peripherally by decreasing the rate of gastric
emptying
d) increasing in the gut peristalsis
e) May produce oculogyric (extrapyramidal) side effect
4- Atropine (all true except one)
a) has vagal inhibition
b) CNS depressant
c) Antisialagogues (decrease salivation).
d) The dose of atropine is 0.3 -0.4 mg iv
e) Increases heart rate
5- Remifentanil (all true except one)
a) is a potent ultra-short-acting synthetic opioid given to patients
during surgery for pain relief
b) Remifentanil is a specific mu-type-opioid receptor agonist c)
causes respiratory depression and analgesia .
d) is antagonized by flumazenil.
e) The analgesic effects of remifentanil are rapid in onset and offset. 6-
Pethidine(meperidine) versus morphine (all true except one) a) 1/10th as
potent as Morphine but Efficacy is similar
b) less miosis, constipation and urinary retention
c) Rapid but short duration of action (2-3 Hrs)
d) antitussive action
e) Less histamine releases
7- Ondansetron (all true except one)
a) Ondansetron is a selective 5-HT3 serotonin-receptor antagonist b)
 used for its antiemetic properties .
c) Ondansetron acts both centrally and peripherally to prevent and
treat nausea and vomiting.
d) has effects peripherally by acting on the laryngeal nerve. e)
The peripheral actions of ondansetron are thought to be the
predominant mechanism for its antiemetic effects.
8- Midazolam (all true except one)
a) is a benzodiazepine

b) It is water soluble at pH< 4 but becomes highly lipid soluble at

physiologic ph.
c) Water solubility minimizes pain at the injection site.
d) Midazolam is more potent, has a faster onset and shorter duration of
action than diazepam.
e) The elimination half-life is 20 hours as against approximately 1.5 t0
3.5 hours in case of diazepam
9- Anxiolytic drugs (all true except one)
a) They act predominantly on GABA receptors
b) Minimum cardiac and respiratory depression
c) Do not produce nausea and vomiting
d) Good analgesic effect
e) Cross the placenta and may cause neonatal depression
10- All the following drugs has analgesic effects except one a)
Clonidine
b) Paracetamol
c) Fentanyl
d) Pethidine
e) Midazolam