PRACTICAL APPLICATIONS OF THE AUTONOMIC DRUGS

ADRENERGIC DRUGS

I. THEORETICAL PART

CLASSIFICATION

Sympathomimetic drugs
 Direct acting
o Non-selective:
 a1 a2 β1 β2: ADRENALINE (Epinephrine)
 a1 a2 β1: NORADRENALINE (Norepinephrine)
 β1 β2 : ISOPRENALINE
o Selective:
 a1 : PHENYLEPHRINE, METHOXAMINE, XYLOMETAZOLINE
 a2 : CLONIDINE, GUANABENZ, GUANFACINE, METHYLDOPA
 β1 : DOPAMINE, DOBUTAMINE
 β2 : SALBUTAMOL, SALMETEROL, TERBUTALINE,
FORMOTEROL, FENOTEROL, METAPROTERENOL,
CLENBUTEROL
 Mixed acting
o a1 a2 β1 β2, releasing agent: EPHEDRINE
 Indirect acting
o releasing agents: AMPHETAMINE, TYRAMINE
o uptake inhibitor: COCAINE
o MAO/COMT inhibitors: PARGYLINE, ENTACAPONE
Sympatholytic drugs
 Alpha-blockers
o Synthetic:
 Non-selective agents (a1 and a2): PHENTOLAMINE,
PHENOXYBENZAMINE, TOLAZOLINE
 Selective agents (a1): DOXAZOSIN, PRAZOSIN, TERAZOSIN
o Natural: ergot alkaloids: ERGOTAMINE, DIHYDROERGOTAMINE,
ERGOTOXINE, DIHYDROERGOTOXINE, ERGOMETRINE,
METHYLERGOMETRINE
 Alpha- and beta-blockers: LABETOLOL
 Beta-blockers

GENERAL PRINCIPLES OF ADMINISTRATION

1. Adrenaline is a drug which can be administered SC (0.1-0.5 ml), IM (onset of action

3-10 min, peak 20 min, duration 20-30 min), IV(0.1-0.25 ml; onset of action
immediate, peak 2-5 min, duration 5-10 min), intracardial or local;
2. Adrenaline is useful in the emergency systemic treatment of anaphylactic shock,
bronchial asthma crisis, cardiac arrest, or local in epistaxis, conjunctivitis, rhinitis or in
association with Lidocaine;
 3. Special precautions have to be considered due to possible side effects after Adrenaline
administration: nausea, vomiting, tremor, agitation, insomnia, dizziness, pallor, HBP,
stroke, arrhythmias (ventricular fibrillation), dyspnea and pulmonary edema;
4. Noradrenaline is administered: IV (4 mg in 250-500 ml Dextrose 5% in water or
normal saline solution infused initially 8-12 g/min, then 4 g/min) in serious acute
hypotensive states to vascular collapse, with systolic blood pressure less than 50
mmHg. The blood pressure should be closely monitored every 2-5 min during
infusion;
5. Adverse effects after Noradrenaline administration could be: anorexia, palpitations,
headache and HBP;
6. Isoprenaline is administered: SL (10-20 mg t.i.d.), IV (0.01-0.02 mg or infusion 2-20
g/min), inhalatory (1-2 puffs every 4-6 h) in congestive heart failure or bronchial
asthma crisis. Tachycardia is a side effect;
7. Phenylephrine can be administered: nasal instillation (2-3 sprays or drops of 0.25-
0.5%) in patients with nasal congestion in patients with common cold, sinusitis,
allergic rhinitis, or IM, IV in hypotension. Other drugs used as local vasoconstrictors
are: Xylometazoline and Ephedrine;
8. Clonidine can be administered: orally (0.2-0.4 mg daily), local (transdermal patches –
0.1-0.2 mg daily), IM, IV, in anxiety, panic disorder, insomnia, Tourette syndrome,
withdrawal symptoms after narcotics, alcohol, nicotine or migraine. Blood pressure
fluctuations, dizziness, nausea, dry mouth could appear as adverse effects.
9. Dopamine is administered in heart failure or shock (except hypovolemic shock). At
doses of 2-10 μg/kg/min, the predominant action is inotrope positive, but at 10-20
μg/kg/min, more vasopressant. Possible side effects are: HBP, tachycardia, skin
necrosis;
10. Dobutamine is administered only IV (5-20 μg/kg/min), in patients with acute
congestive heart failure or after heart surgery;
11. Phentolamine, Phenoxybenzamine and Tolazoline have limited indication to
feocromocytoma;
12. Doxazosin, Prazosin and Terazosin are administered in HBP, but may produce low
blood pressure, especially after the first administrations;
13. Ergot alkaloids are useful as vasodilators (Ergotoxine, Dihydroergotoxine),
vasoconstrictors (Ergotamine, Dihydroergotamine) or oxytocics (Ergometrine,
Methylergometrine);
14. Beta-blockers are used in the treatment of HBP, arrhythmias, cardiac ischemia, heart
failure or glaucoma (local administration).

TREATMENT OF ANAPHYLACTIC SHOCK

Anaphylaxis is a medical emergency that requires immediate recognition and intervention.
Untreated it may lead to the death of your patient. Basic equipment and medication should be
readily available in the physician’s office.
Causes:
 Drugs: penicillin
 Insect sting, snake bite
 Radiocontrast media
 Food: peanuts, shellfish, milk, eggs
 Latex
 Rare: physical effort
Risk factors:
 a previous anaphylactic reaction
  allergies or asthma
 a family history of anaphylaxis
Treatment:
 Remove the source of the antigen, if possible: stop drug administration, remove
stinger after honeybee sting
 High-flow oxygen
 Place the patient in a supine position (or position of comfort if dyspneic or vomiting)
with the legs elevated.
 Check the airway
 Cardiac monitoring, pulse oximetry
 IV access; administer physiological serum. A keep-vein-open (KVO) rate is
appropriate for patients with stable vital signs and only cutaneous manifestations. If
hypotension or tachycardia is present, administer a fluid bolus 1 L. Further fluid
therapy depends on patient response.
 Epinephrine:
o is the drug of first choice in anaphylactic shock, whith lifesaving potential
(anaphylactic deaths correlate with delayed administration of epinephrine)
o immediately 0,3-0,5 mg IM, in the thigh, repeated as necessary, depending on
the response
o maintains blood pressure
o antagonizes the effects of the released mediators and inhibits further release of
mediators
o via a nebulizer can be used to reduce laryngeal swelling, but it does not replace
IM administration of epinephrine
o if bronchospasm has not responded to IM epinephrine, administer inhaled beta 2
-adrenergic agonists (albuterol)
 Corticosteroids:
o Hydrocortisone 100-200 mg IV, increase dose if necessary
o Prednisone 20-80 mg/day orally for 2-5 days
 H1 blocker and an H2 blocker:
o the combination is superior to an H1 blocker alone, in relieving the histamine-
mediated symptoms
o Diphenhydramine: 25 mg orally (IV) every 6 hours for 2-5 days
o Ranitidine: 150 mg orally or 50 mg IV
o bronchial asthma crisis.

Preparations

Generic drug Brand name Route of Pharmaceutical

administratio dosage form
n
Adrenaline Adrenaline s.c, IM, IV vial 1 ‰, 1ml
EpiPen IM prefilled pen
0,15 mg; 0,3 mg
Noradrenaline Noradrenaline Tartrate PEV conc. sol. inf.
Aguettant 0,2%, vial 4ml,
8ml
Dopamine Dopamine Admeda PEV conc. sol. inf.
 20mg/ml, vial
10ml
Dopamine clorhidrat PEV conc. sol. inf.
5mg/ml, vial
10ml
Xylometazoline Bixtonim Xylo intranasal Nasal drops
0,5mg/ml,
Olynth 1mg/ml; nasal
spray 1mg/ml
Phenylephrine Coldrex Lemon p.o. Powder for oral
(paracetamol+ susp.
phenylephrine +
ascorbic acid)
Ibuprofen/Clorhidrat p.o. tab 200 mg/5 mg
of Phenylephrine
Zentiva
Clonidine Clonidine p.o. tab 0,15 mg
Isoprenaline Bronhodilatin SL, SC, IM, tab subling. 10
IV, PEV mg, vial
0,2mg/1ml
Novodrin inhalator aerosoles 0,5%
Dobutamine Dobutamida Admeda PEV vial 50mg/250ml
Ephedrine Efedrina IV vial 50mg/1ml
Ser efedrinat intranasal Nasal drops 0,5%;
1%
Phenoxybenzamine Fenoxibenzamina p.o. tab 10 mg
Tolazoline Tolazolin p.o., IM, IV, tab 25mg, vial
i.a. 10mg/1m
Phentolamine Regitine p.o., IV tab 50mg, vial
10mg/ml
Prazosin Minipress p.o. tab 1 mg, 5 mg
Terazosin Terazosin p.o. tab 1mg, 2mg,
5mg
Doxazosin Cardura p.o. tab 1,2 mg
Aniprosin p.o. tab 2 mg, 4 mg
Ergotoxine Ergoceps p.o. int. sol. 1mg/ml
Dihidroergotoxine Redergin p.o. int. sol. 1mg/ml
Ergotamine Cofedol p.o. dj.1mg
ergotamine + 100
mg coffein
Dihidroergotamine Cornhidral p.o. int. sol. 2mg/ml
Migranal intranasal spray nasal 0,5
SC, IM, IV mg/puff, vial
1mg/1ml
Ergometrine Maleat de ergometrină IM, IV vial 0,2 mg/ml
Metilergometrine Metilergometrina p.o. dj. 0,125 mg,
 maleat IM, IV vial 0,2mg/1ml

II. PRACTICAL PART

1. Write a medical prescription to a patient with cerebral aterosclerosis and symtoms of
imbalance.
2. Write a medical prescription to a patient with HBP.
3. Write a medical prescription to a patient with migraine.
4. A patient of 80 kg with cardiogenic shock receives Dopamine IV infusion 5
μg/kg/min. Calculate the rythm of administration in ml/hours.
Available: Dopamine vial 50 mg/10 ml. Syringe pump of 100 ml (1 vial of Dopamine
in Physological serum).