Key Names and stuff

• Albumins

  • Mostly bind acid(low pKa) xenobiotics

  • Two bindings sites

  • Low specificity

  • Bind many endogenous compounds(steroids/hormones)

• Acid ã 1-glycoproteins

  • Binds basic xenobiotics(higher pKa)

  • One binding site(disadvantage)

Hemoprotein Cytochrome P450

GABA

Barbiturates

Dopamine receptors - they block the Dopamine D2 receptor, changing the threshold of excitability - agonists

Sedation/tranquilization/vomiting prevention

Anxiolytics

GABA

Benzodiazepines, compared to others

Ketamine

Sedation, minor muscle relaxation, anticonvulsant activity

Benzodiazepines

• Diazepam(Valium)

• Midazolam

• Alprazolam(Xanax)

• Phenothiazine derivatives

• Benzodiazepine derivatives

• Alpha2-adrenergic agonists

They block pre-synaptic a2 receptors(blockthe release) and use negative feedback mechanism

Atipamezole

• Xylazine and ketamine

• Xylazine and butorphanol

• Morphine and acepromazine

• Oxymorphone ans acepromazine

• Fentanyl and droperidol

Opioid antagonists

Propofol - no analgesic effect, needs it added. Short validity, needs to be re-induced.

Analeptics/stimulants

• Doxapram - activates respiratory centers

• Caffeine - cardiokinetic/slight diuretic/slight antidepressant

• Theobromine - diuretic

• Theophylline - cardiokinetic/bronchodilator

• Adenosine receptors antagonists

• Inhibit degradation of cAMP and cGMP

• Naloxone

• Nalorphine

Antidotal treatments for overdose of opioids

• Ketamine

• Tiletamine

Dissociative agents

• Mu(1&2)

• Delta(1&2)

• Kappa

• Sigma

• Tranquilizers - sedation/calm

• Barbiturates - intravenous, anti-seizure(epilepsy)

• Dissociatives - anaesthetics(ketamine)

• Opioids and antagonists(morphine)

• Neuroleptoanalgesics

• Euthanasia agents

• CNS stimulants

1. Long acting - phenobarbital

2. Short acting - phentobarbital

3. Ultrashort acting - thiobarbiturates

Thiobarbiturates

No, but they stop ventilation(manual needed) and are usually adjunct to general anaesthesia

• Depolarizing

• Non depolarizing

Ionotropic

• Non depolarizing agents

• Neostigmine

Pentobarbital

Intratracheally

• Carbon monoxide

• Carbon dioxide(above 60%)

• NSAIDs

• Opioid Analgesics

• Corticosteroids

• Local anesthetic agents

• Others

• Corticosteroids block Phospholipase A2 through the action of lipocortin and this stops the synthesis of all: thromboxane, leukotrienes ans prostaglandins

• NSAIDs block cyclooxygenase(COX)

Arachnidonic acid

• COX 1 - renal blood flow, synthesis of gastric mucosa - side effects if inhibited by NSAIDs

• COX 2 - induced by tissue injury, promotes the formation of prostaglandins - inhibition goal of NSAIDs

Cyclooxygenase

To reduce both inflammation and pain

Only COX 1, or tiny amounts of COX 2(it is activated by inflammation process)

• Aspirin

• Ibuprofen, naproxen

• Meloxicam, sulindac, nabumetone

• Celecoxib, firococxib

• Aspirin

• Phenyl Butazone

• Flunixin Meglumin

• Acetamenophen(Paracetamol) - very toxic for cats

• Buscopan

• Caprofen

• Ketaprofen/Ibuprofen

• Osteoarthritis associated drugs

• Natural compounds - too potent, not used, active for less than 12h

• Synthetic compounds - fluorine increases lipophilicity and stability, 12-36h of action(or even 2 days)

• There are also mineral corticoids, which deal with regulation of water/electrolyte balance and act as agonists for M receptors in kidneys

Glucocorticoids

• Mineralocorticoids

• Glucocorticoids

They act on glucocorticoids receptors, which triggers intracellular protein synthesis, which produces Lipocortin, which inhibits Phospholipase A

By inducing desensitization of the nerve: they prevent action potential conduction through the blockage of Ionotropic Na+ channels - no sensory signal.

Blocking of downstream nervous impulses

• According to structure(lipophilicity) and potency(length of the C chain)

• According to binding:

  • Ester-like drugs - less potent, can be administered through infiltration

  • Amide-like drugs - most commonly used(Lidocaine, bupivacaine)

Systemic effect - when not local anymore

• Anxiety

• Hypotension

• Lidocaine(faster onset)

• Bupivacaine(longer lasting)

• Loop

• K-sparing

• Thiazide-like

• Carbonic Anhydrase inhibitors

Caffeine - inhibitor of phosphodiesterase, antagonist of adrenergic receptors.

It inhibits sodium reabsorption

1. Acetazolamide(proximal)

2. Mannitol(proximal)

3. Loop diuretics(loop of Henle)

4. Thiazide diuretics(distal)

5. Aldosterone antagonist(collection duct)

Mostly Na or Na tied particles excretion into the lumen, attracting the water.

• Hypokalemia - deficit of K in blood because of increased excretion by loop diuretics, carbonic Anhydrase inhibitors, thiazide diuretics

• Hyperkalemia - as a result of concurrent administration of potassium supplements when taking aldosterone antagonists(reduced excretion of K, M receptor)

1. Loop diuretics

   • Excrete: Cl, K, H2O

   • Inhibit absorption: Na

2. Thiazide diuretics

   • Excrete: NaCl

   • Reduce the K loss

3. Acetazolamide(carbonic anhydrase inhibitors)

   • Excrete: sodium bicarbonate(no Na - acidosis) , solutes(indirectly through involvement in dissociation of carbonic acid)

   • Inhibit absorption: bicarbonate

• Ammonium chloride

• Sodium bicarbonate

Both given orally

• D: loss of K+

• V: loss of K+ and Cl-

• Dry oral mucous membranes

• Increased skin tenting(skin turgor test)

• Tachycardia

• Decreased pulse pressure

• Sunken eyes

• Alteration of consciousness

Lab diagnosis tests:

• ↑ Packed cell volume

• ↑ Total plasma protein

• ↑ Urine specific gravity determination

• Hypotension

• Tachycardia

• Hypothermia

• Weak peripheral pulses/cooling of peripheral extremities

• Pale mucous membranes

1. Hydration deficit

   • Fluid to be replaced to come to the norm

   • %dehydration × normal body weight = kg ->ml

2. Maintenance value

   • For smooth readaptation

   • (30 × kg bw) + 70 = ml/day

3. Contemporary(ongoing) losses

   • 100 ml for the ongoing puking/diarrheing

All added together = amount of fluid therapy to be given

• Colloids

  • Synthetic starch-based colloids

  • Natural colloids

• Crystalloids

  • Isotonic high-sodium(replacement solutions)(resemble ECF)

  • Hypotonic low-sodium(maintenance solutions)(more K)

  • Hypertonic saline solutions

• Mixture of crystalloids

(Volume to be administered (mL) ÷ Time of infusion (min))× drop factor(drops/mL)

• 15 drops/mL - macrodrip

• 60 drops/mL - microdrip

Hypertonic

They have a higher osmolality than ECF(more things inside) and so they absorb H2O from there into the blood.

Should be associated with the use of diaretics to clean blood of excessive fluids

• Apomorphine - CTRZ receptors, bad for felines

• Xylazine - alpha-2 antagonist, good for felines

Locally acting emetics

• NaCl

• Ipecac - peristaltic waves, prokinetic, anti bloating

• Hydrogen peroxide - 4% solution orally, takes 5-10 minutes

• Phenothiazine Derivatives - D2 antagonists

  • Chlopromazine - not so good for cats

  • Prochlorperazine - less sedative

  • *Metoclorpramide(Reglan) - for chemotherapy, short half-life, continuous drip

• Antihistamines(H1 Blockers) - Benadryl, Dramamine

• Serotonin Receptors(5-HT3) antagonists - chemotherapy, expensive

• NK-1 Receptor Antagonists - motion sickness

Bad: sedation, hypotension, *behavioral disorders

• H2 receptor antagonists -Block H2 and ↓ gastric HCL release, over the counter,

  • Cimetidine - least potent, short half life(3-4 times/day), inhibits liver microsomal enzymes, thus hindering rate of metabolism of other drugs, needs low pH

  • Ranitidine(Zantac) - little effect on liver/little drug interactions, 5 times more potent, prokinetic

  • Famotidine - better than both, but expensive

• Proton pump inhibitors - bind irreveesibly to Na/K ATPase pump and inhibit release of H ions; pro drugs(metabolicly activated) by P450(CYP1A1, CYP1A2), might provoke constipation, headache, rush

  • Omeprazole

  • Lansoprazole

  • Pantoprazole

• Antacids(local) - calm irritation from HCl, chelating action(get rid of excess Phosphorus), might give constipation and should be taken in advance before other oral medications

  • Maalox- Magnesium, Aluminum

• Gastromucosal protectants - disaccharide- protective layer on the ulcer, physical protection, given before other drugs but followed by 1 and 2 group medications

  • Sucralfate - the only one used in vet medicine

• Prostaglandin E1 analogues

  • Misoprostol - the only one used, must be combined with others, ↑ bicarbonate(so ↓ the pH). Protects against long use of NSAIDs. NOT IN PREGNANT ANIMALS

• Narcotic analgesics(opiates)

  • Loperamide(Imodium) - doesn't penetrate CNS, might interact with other drugs. Sedation, constipation

  • Diphenoxylate(Lamutile)

• Anticholinergic/Antispasmodics - M3 receptor in GI tract

  • Buscopan

• Protectants/adsorbents - constipation

  • Activated charcoal - absorbs substances and toxins

  • Kaolin and Pectin

  • Bismuth subsalicylate - releases Aspirin, anti inflammatory/antibacterial effect, inhibit the release of prostaglandins, black-red faeces

• Saline/hyperosmotic agents - liquid recall, cramping/nausea

  • Lactulose

  • Magnesium hydroxide

  • Milk of magnesia and epsom salts

• Bulk-producing - liquid absorbing

  • Psyllium preparations

• Lubricants - better interaction between stool and mucosa

  • Mineral oils

  • Petrolatum

• Surfactants/stool softeners - simpler defecation, loss of micronutrients

  • Docusate sodium

• Irritants - irritate the muscles to contract

  • Bisacodyl(Dulcolax)

• Dopaminergic antagonists - antiemetics, prokinetics

  • Domperidone

  • Metochopramide

• Serotoninergic drugs

  • Cisapride - diarrhea, abdominal pain(when too much)

• Motilin-like drugs

  • Erythromycin - motilin receptor agonist, antibiotic, poorly absorbed, so only local inside. Vomiting and diarrhea

• Acetylcholinesterase inhibitors - block acetylcholinesterase. Nausea, vomiting, diarrhea

  • Neostigmine

  • Ranitidine - agonist of H2, prokinetic effect

• Nebulizers

• MDI - Metered Dose Inhalers

Include bronchodilators and mucolytics

Also sometimes corticosteroids

More viscous mucus from the lungs

• Guaifenesin

• Iodine preparations

• Hypertonic saline

It provokes nausea and vomiting when administered orally because of bad taste and smell

• Butorphanol Tartrate - opioid mixed agonist and antagonist for m receptors

• Codeine - drug of abuse

• Dextromethorphan - not of abuse, syrup, acts on cough centre in medulla

• Temaril-P

Selective toxicity - not attacking the host

• Nematodes - Cholino-mimetic, act on GABA and Glutamate receptors

• Cestodes - Cholino-mimetic, digestion of parasite

• Trematodes - blocking ATP synthesis

• Antiprotozoal - act on larvae replication

On:

• Nucleus - cytoskeletal protein, DNA synthesis inhibited

• Cell membrane/wall - membrane permeability altered

• Cell wall - no chitin synthesis

• Cell wall

• Cell membrane

• 2 ribosome subunits

• 1 ribosome subunit

• Nucleic acid

• DNA

• Folic acid Synthesis pathway