NEET MDS Lessons
Pharmacology
ANTICHOLINERGIC DRUGS
Blocks the action of Ach on autonomic effectors.
Classification
Natural Alkaloids - Atropine. Hyoscine
Semi-synthetic deriuvatives:- Homatropine, Homatropine methylbromide, Atropine methonitrate.
Synthetic compounds
(a) Mydriatics - Cyclopentolate. Tropicamide.
(b) Antisecretory - Antispasmodics - Propantha1ine. Oxy-phenonium, Pirenzipine.
c) Antiparkinsonism- Benzotopine, Ethopropazine, Trihexyphenidyl, Procyclidine, Biperiden
Other drugs with anticholinergic properties • Tricyclic Antidepressants • Phenothiazines • Antihistaminics • Disopyramide
MUSCARINIC RECEPTORS SUBTYPES & ANTAGONISTS
• M 1 Antagonists – Pirenzepine, Telenzepine, dicyclomine, trihexyphenidyl
• M 2 Antagonists – Gallamine, methoctramine
• M 3 Antagonists – Darifenacin, solifenacin, oxybutynin, tolterodine
Pharmacological Actions
CNS - stimulation of medullary centres like vagal. respiratory. vasomotor and inhibition of vestibular excitation and has anti-motion sickness properties.
CVS - tachycardia.
Eye - mydriasis
Smooth muscles - relaxation of the muscles receiving parnsympathetic motor innervation.
Glands - decreased secretion of sweat and salivary glands
Body Temperature - is increased as there is stimulation of temperature regulating centre.
Respiratory System- Bronchodilatation & decrease in secretions. For COPD or Asthma - antimuscarinic drugs are effective
GIT - Pirenzepine & Telenzepine - decrease gastric secretion with lesser side effects.
DOPAMINE
It is an immediate metabolic precursor of noradrenaline. It activates D1 receptors in several vascular beds, which causes vasodilatation. It acts on dopaminergic and other adrenergic receptors (α & β1).
Adverse effects of dopamine include nausea, vomiting, ectopic beats, anginal pain, tachycardia, palpitation and widened QRS.
Contraindications are atrial or ventricular tachyarrhythmias, hyperthyroidism and pheochromocytoma.
Cephalosporins
Produced semisynthetically by chemical attachment of side chains to 7-aminocephalosporanic acid. Same mode of action , same resistance mech.
But tend to be more resistant than penicillins to certain beta –lactamases .
GENERATION BASED ON :
-- BACTERIAL SUSCEPTIBILITY PATTERNS
-- RESISTANCE TO BETA –LACTAMASES
--NOT EFFECTIVE AGAINST -MRSA , L. MONOCYTOGENES , C. DIFFICLE , ENTEROCOCCI
First Generation
Parentral
- CEPHALOTHIN
- CEFAZOLIN
Oral
- CEPHALEXIN
- CEPHRADINE
- CEFADROXIL
Second Generation
Parentral
CEFUROXIME
CEFOXITIN
Oral
CEFACLOR
CEFUROXIME AXETIL
Third Generation
Parentral
CEFOTAXIME
CEFTIZOXIME
CEFTRIAXONE
CEFTAZIDIME
CEFOPERAZONE
Oral
CEFIXIME
CEFPODOXIME
CEFDINIR
CEFTIBUTEN
Fourth Generation
Parentral
CEFEPIME
CEFPIROME
Oxycodone
About equal potency to morphine. Very effective orally.
It is combined with aspirin or acetaminophen for the treatment of moderate pain and is available orally
Oxycodone is a semisynthetic compound derived from thebaine, with agonist activity primarily at mu receptors.
ISOPRENALINE
It is beta-receptor stimulant, which stimulates the heart and causes tachycardia.
It relaxes the smooth muscles particularly the bronchial and GIT. It is mainly used in bronchial asthma, in the treatment of shock and as a cardiac stimulant in heart block.
ORCIPRENALINE
Is a potent β-adrenergic agonist.
Receptor sites in the bronchi and bronchioles are more sensitive to the drug than those in the heart and blood vessels.
AMPHETAMINE
increases the systolic and diastolic blood pressure. Amphetamine is a potent CNS stimulant and causes alertness, insomnia, increased concentration, euphoria or dysphoria and increased work capacity.
Amphetamines are drugs of abuse and can produce behavioural abnormalities and can precipitate psychosis.
PHENYLEPHRINE
It is used as a nasal decongestant and mydriatic agent and also in the treatment of paroxysmal supraventricular tachycardia.
UTERINE RELAXANTS (TOCOLYTICS)
ISOXSUPRINE
Isoxsuprine has a potent inhibitory effect on vascular and uterine smooth muscle and has been used in the treatment of dysmenorrhoea, threatened abortion, premature labour and peripheral vascular diseases.
Gentamicin
Gentamicin is a aminoglycoside antibiotic, and can treat many different types of bacterial infections, particularly Gram-negative infection.
Gentamicin works by binding to a site on the bacterial ribosome, causing the genetic code to be misread.
Like all aminoglycosides, gentamicin does not pass the gastro-intestinal tract, so it can only be given intravenously or intramuscularly.
Gentamicin can cause deafness or a loss of equilibrioception in genetically susceptible individuals. These individuals have a normally harmless mutation in their DNA, that allows the gentamicin to affect their cells. The cells of the ear are particularly sensitive to this.
Gentamicin can also be highly nephrotoxic, particularly if multiple doses accumulate over a course of treatment. For this reason gentamicin is usually dosed by body weight. Various formulae exist for calculating gentamicin dosage. Also serum levels of gentamicin are monitored during treatment.
E. Coli has shown some resistance to Gentamicin, despite being gram-negative
Ketoconazole
synthetic antifungal drug
used for infections such as athlete's foot, ringworm, candidiasis (yeast infection or thrush), jock itch.
Ketoconazole is used to treat eumycetoma, the fungal form of mycetoma.
MOA: Ketoconazole is imidazole structured, and interferes with the fungal synthesis of ergosterol, the main constituent of cell membranes, as well as certain enzymes. It is specific for fungi, as mammalian cell membranes contain no ergosterol.
Sensitive fungi Ketoconazole inhibits growth of dermatophytes and yeast species (such as Candida albicans).