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Pharmacology - NEETMDS- courses
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Pharmacology

Local Anesthetics

1. Procaine (Novocaine)

a) Classic Ester type agent, first synthetic injectable local anesthetic.

 b) Slow onset and short duration of action

 2. Tetracaine (Pontocaine)

a) Ester type agent--ten times as potent and toxic as procaine.

 b) Slow onset but long duration of action.

 c) Available in injectable and topical applications.

 3. Propoxycaine (Ravocaine)

a) Ester type agent–five times as potent and toxic as procaine.

 b) Often combined with procaine to increase duration of action.

 4. Lidocaine (Xylocaine)

a) Versatile widely used amide type agent.

 b) Two - three times as potent and toxic as procaine.

 c) Rapid onset and relatively long duration of action.

 d) Good agent for topical application.

 5. Mepivacaine (Carbocaine)

a) Amide type agent similar to lidocaine.

 b) Without vasoconstrictor has only short duration of action.

6. Prilocaine (Citanest)

a) Amide type agent — less potent than lidocaine.

 b) Without vasoconstrictor has only short duration of action.

 c) Metabolized to o-toluidine which can cause methemoglobinemia — significant only with large doses of prilocaine.

 d) Higher incidences of paresthesia reported with 4 % preparation

7. Bupivacaine (Marcaine)

a) Amide type agent of high potency and toxicity.

 b) Rapid onset and very long duration of action even without vasoconstrictor.

 8. Articaine (Septocaine)

a) Amide type agent

 b) Only amide-type local anesthetic that contains an ester group, therefore metabolized both in the liver and plasma.

 c) Approved by the FDA in 2000

 d) Evidence points to improved diffusion through hard and soft tissues as compared to other local anesthetics.

 e) Reports of a higher incidence of paresthesia, presumably due to the 4% concentration

 f) Not recommended for use in children under 4 years of age

 

Cough is a protective reflex which helps in expulsion of respiratory secretion or foreign particles which are irritant to respiratory
tract. Irritation to any part of respiratory tract starting from pharynx to lungs carried impulses by afferent fibres in vagus and
sympathetic nerve to the cough centre in the medulla oblongata. \

Cough may be dry (without sputum or unproductive) or productive (with sputum production). 


Classification for drugs used in cough.

I. Pharyngeal demulcents

Certain lozenges, linctus and cough drops containing glycerine, liquorice and syrups.

II. Expectorants

Sodium and potassium citrate
Sodium and potassium acetate 
Potassium iodide 
Ammonium chloride & carbonate
Acetylcysteine 
Bromhexine 
Guaiphenesin 


III. Antitussive

i. Opioids

Codeine (as linctus) Pholcodeine 

ii. Non-opioids

Noscapine
Dextromethorphan
Pipazethate 

iii. Antihistaminics

Chlorpheniramine 
Diphenhydramine 
Promethazine

Erdosteine is recently introduced mucolytic with unique protective functions for the respiratory tract. It is indicated in the treatment of acute and chronic airway diseases such as bronchitis, rhinitis, sinusitis, laryngopharyngitis and exacerbations of chronic bronchitis.

Use of local anesthetics during pregnancy

Local anesthetics (injectable)

Drug                                                   FDA category

Articaine                                             C

Bupivacaine                                        C

Lidocaine                                            B

Mepivacaine                                        C

Prilocaine                                            B

Vasoconstrictors

Epinephrine 1:200,000 or 1:100,000 C (higher doses)

Levonordefrin 1:20,000 Not ranked

Local anesthetics (topical)

Benzocaine                                        C

Lidocaine                                            B

Monoamine oxidase inhibitors (MAOIs) 

e.g. phenelzine, tranylcypromine, moclobemide

- Belong to first generation antidepressants with TCAs
- Most MAOIs irreversibly inhibit the intraneuronal catabolism of norepinephrine and serotonin by MAO-A and MAO-B
- increase brain levels of noradrenaline and 5-HT
- Moclobemide causes selective, reversible inhibition of MAO-A

DRUG INTERACTIONS

Hypertensive crises similar to cheese reaction with OTC cough/cold preparations containing indirect-sympathomimetics
e.g. ephedrine

- Other antidepressants should not be started at least 2 weeks after stopping MAOIs and vice versa due to risk of serotonin syndrome
- Similar interaction with pethidine

ADVERSE DRUG REACTIONS

- Antimuscarinic side effects (e.g. dry mouth, blurred vision, urinary retention)vision, urinary retention)
- Excessive central stimulation causes tremors, excitement and insomnia
- Postural hypotension
- Increased appetite with weight gain

Quinolone

Quinolones and fluoroquinolones form a group of  broad-spectrum antibiotics. They are derived from nalidixic acid.

Fluoroquinolone antibiotics are highly potent and considered relatively safe.

MOA : Quinolones act by inhibiting the bacterial  DNA gyrase enzyme. This way they inhibit nucleic acid synthesis and act bacteriocidically.

Drugs  :Nalidixic acid, Ciprofloxacin , Levofloxacin,  Norfloxacin ,Ofloxacin,  Moxifloxacin  , Trovafloxacin

Carbapenems: Broadest spectrum of beta-lactam antibiotics.

imipenem with cilastatin

meropenem

ertapenem

Monobactams: Unlike other beta-lactams, there is no fused ring attached to beta-lactam nucleus. Thus, there is less probability of cross-sensitivity reactions.

aztreonam

Beta-lactamase Inhibitors No antimicrobial activity. Their sole purpose is to prevent the inactivation of beta-lactam antibiotics by beta-lactamases, and as such, they are co-administered with beta-lactam antibiotics.

clavulanic acid

tazobactam

sulbactam

Serotonin or 5-hydroxytryptamine (5-HT)

It is a neurotransmitter, widely distributed in the CNS, beginning in the midbrain and projecting into thalamus, hypothalamus, cerebral cortex, and spinal cord. CNS serotonin is usually an inhibitory neurotransmitter and is associated with mood, the sleep-wake cycle.

Serotonin is thought to produce sleep by inhibiting CNS activity. 

In the blood, 5-HT is present in high concentration in platelets (regulator of platelets function) and also high concentration in intestine

Pharmacological effects:

Smooth muscles. 5-HT stimulates the G.I smooth muscle; it increases the peristaltic movement of intestine.
Serotonin contracts the smooth muscle of bronchi; 

Blood vessels. If serotonin is injected i.v, the blood pressure usually first rises, because of the contraction of large vessels and then falls because of arteriolar dilatation. Serotonin causes aggregation of platelets. 

Specific agonists

- Sumatriptan a selective 5-HT1D used in treatment of acute migraine.
- Buspirone a selective 5-HT1A used in anxiety.
- Ergotamine is a partial agonist used in migraine. It acts on 5-HT1A receptor.

Nonspecific 5-HT receptor agonist

o Dexfenfluramine used as appetite suppressant.

Specific antagonists

o Spiperone (acts on 1A receptor) and
o Methiothepin (acts on 1A, 1B, 1D receptors)

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