Penicillin, Amoxicillin, and Cephalosporin Classes

Penicillin Class

• Narrow-spectrum antibiotics.
• Penicillin V is administered orally, and the chalky suspension is underutilized due to its poor taste.
• Adverse effects include GI upset, nausea, vomiting, diarrhea, and rash.
• True penicillin allergy is a rare occurrence.
• This class is considered drug of choice for Group A Streptococcal Pharyngitis.

Amoxicillin

• Extended-spectrum penicillin.
• It is essentially a modified version of penicillin that results in greater activity against additional gram-negative bacteria.
• More well-tolerated, but can have same adverse effects.
• Typically used more often as it is more palatable

Cephalosporin Class

• Greater structural diversity, more resistant to beta-lactamases, and increases range of anti-microbial activity.
• More resistant to resistance mechanisms of bacteria.
• Cefadroxil is a first-generation cephalosporin.
• It is used if treatment failure with penicillin or in individuals with non-immediate hypersensitivity to penicillin's.
• Adverse effects include GI upset, nausea, vomiting, diarrhea, hypersensitivity, and some cross-reactivity with penicillin's.
• Cephalexin is first generation cephalosporin.
• It presents same adverse effects as above.
• It is available as a suspension.

Macrolides Class

• Inhibit peptidyl transferase which functions to link amino acids in growing peptide chain.
• Interferes with translocation and confers bacteriostatic activity (NOT bactericidal).
• Azithromycin is an alternative for patients allergic to penicillin.
• Less likely than other macrolide antibiotics to interact with other drugs.
• Adverse effects include GI upset, nausea, vomiting, diarrhea, rash and QTc interval prolongation.
• Clarithromycin is an alternative for patients allergic to penicillin
• Presents same adverse effects as above
• Available in suspension
• Increases levels of some common drugs (i.e., statins and prednisone)

Lincosamides Class

• Interfere with translocation like macrolides, but do not inhibit peptidyl transferase.
• Approximately 4x more likely to cause C. difficile infections compared to other antibiotics.
• Generally bacteriostatic, but high doses are bactericidal.
• Clindamycin is an alternative for those allergic to penicillin
• May be for treatment in symptomatic patients with multiple, recurrent episodes of penicillin.
• Commonly causes diarrhea as adverse effect.
• Wirth regards to strep throat, antibiotics reduce duration of symptoms by approx. 16 hours
• Small benefit given, antibiotic therapy could be withheld for 48-72 hours in adult patients with more severe symptoms

Absorption

• Most drugs absorbed by passive diffusion.
• Some drugs use physiological transport processes.
• Oral drugs normally absorbed in the small intestine after drug goes through first effects in the liver.
• Absorption dependent on route of admin (IV = 100% bioavailable, whereas Oral = modified significantly in first pass before reaching target).
• For orally admin drugs, there are two significant pH compartments in digestive tract (stomach pH is 1 and small intestine pH is neutral).
• The fraction of administered dose of drug that reaches the systemic circulation in an active, unchanged form is bioavailability.
• Drugs are easily metabolized by the liver, formulated in a way so first pass effect is used to ACTIVATE a drug (some)
• Metabolites may retain some degree of pharmacological activity.
• Not every xenobiotic is immediately detoxified (some create MORE toxic intermediate requiring more metabolism before inactivating - liver damage).
• First-pass effect happens when drug is administered, absorbed in digestive tract, then goes to liver via portal vein BEFORE entering systemic circulation.
• Liver can act on drug prior to entering body circulation, and degree to which drug is inactivated by liver enzymes prior to entering the systemic circulation substantially alters the drug's bioavailability.

Distribution

• Size of organ and blood flow are distribution factors.
• Drug solubility is a factor, as fat-soluble drugs or those resembling hormones are very easily absorbed into fat compartments, but don't necessarily float around so well without a chaperone in fluid compartment of blood.
• Protein binding by albumin is the most common circulatory protein, BUT drugs significantly protein bound introduce issues surrounding drug interactions.
• IV drugs are 100% bioavailable by definition.
• SAFE in pregnancy/lactation: Myrrh
• Not all drugs need to be metabolized to be eliminated.
• Not all are inactivated by metabolism
• Prodrugs are activated by metabolism
• Usnic acid is main phytochemical
• Usnic acid is НЕРАТОXIC, may cause drug-induced hepatitis via mitochondrial uncoupling
• Antibiotic therapy generally not recommended for mild cases.
• Both oregano and thyme essential oils are rich in monoterpenes that inhibit Streptococcus pyogenes.
• Affinity for the LEFT side of the body or LEFT -> RIGHT (travels)
• Distribution molecule to the spot opened by phase I reactions.
• Phase II Metabolism is that conjugating something to an available OH group, each phase II mechanism has its own enzyme.
• Glucuronide conjugates are excreted in bile.
• Some commensal gut bacteria have glucuronidase enzymes which can cleave glucuronide off metabolite resulting in parent drug being able to be reabsorbed
• The gut microbiome allows drug to re-enter circulation to have a second effect (cleave off what happened in phase II metabolism).
• Very important in most water-soluble drug metabolites being the kidneys.
• Various mechanisms exist throughout sections of nephron for doing this.
• Lipid-soluble drugs excreted in distal tubule if they're small enough (if large, they enter bile).
• Lipid-soluble drug metabolites and glucuronide-conjugates are excreted by liver into bile and are excreted in feces

Botanical Medicine

• The H.E.M.P Formula includes Hydratis (goldenseal), Echinacea (purple cone flower), Myrrh and Phytolacca (poke root).
• Goldenseal (Hydrastis canadensis) is considered the "King of Mucous Membranes".
• It can be used to counter inflammation and infections of the respiratory and GI tract.
• It is mainly antimicrobial (also antibacterial, antiviral, antifungal, antiparasitic).
• Goldenseal is a digestive bitter, and should not be taken during pregnancy/lactation.
• Goldenseal is CONTRAINDICATED in gastritis and stomach ulcers, obstructed gallbladder.
• SIDE EFFECTS include GI irritation.
• Echinacea purpurea/angustifolia/pallida is immunostimulant (MAIN).
• Echinacea can be used for strep throat, preventing/treating common cold, flu and URIs, vaginal candidiasis, and UTI.
• Main constituents are alkylamides, phenolics, polysaccharides.
• Echinacea CAUTION in auto-immune disease.
• Commiphora myrrha is indicated mainly for tonsilitis and gingivitis.
• Myrrh is mainly antimicrobial (also antibacterial, antiviral, antifungal, antiparasitic).
• Actions can help to cause Analgesic, Expectorant, and Astringent
• Main constituents include oleoresin and sesquiterpenes.
• Myrrh is NOT RECOMMENDED in pregnancy.
• Phytolacca americana main indication is lymphadenopathy
• Main action is lymphatic and with emetic and purgative activity.
• It is a TOXIC herb and may cause violent emesis, catharsis, convulsions and possible death.
• Phytolacca is NOT RECOMMENDED in pregnancy
• Usnea barbata main indication indications are infections.
• Actions include antimicrobial, antibacterial, antiviral, antifungal, and antiparasitic.
• Enterohepatic Circulation with: Glucuronide conjugates (that) are excreted in bile.
• Some commensal gut bacteria have that (glucuronidase) enzymes which can cleave glucuronide off metabolite resulting in parent drug being able to be reabsorbed.
• Therefore, (by) the gut microbiome allows drug to re-enter circulation to have a second effect (cleave off what happened in phase II metabolism where glucuronide was added)

Homeopathy

• Belladonna is #1 remedy for strep throat infection, standing for violence of attack and suddenness of onset.
• Hot (fever), red skin and throat.
• Tonsils enlarged, throat feels constricted and swallowing is difficult .
• Patients experience throbbing, burning and flushed face with glaring eyes, along with throbbing carotids and Excited mental state.
• There is Hyperesthesia of all senses, Delirium and/or Restless sleep.
• Convulsive movements also noted, with Dryness of mouth and throat and aversion to water.
• Better when: Leaning head against something, bending the part back or inward, while standing, in bed, in morning, with warmth.
• VERY THIRSTY and a Fear of death with Panic attack and Numbness and pain.
• Gelsemium has gradual onset of complaints.
• Muscular weakness, muscle aches, soreness, pain, heaviness (noted with Gelsemium patients).
• Gelsemium presents Thirstlessness where patient is:
• "Droopy, dizzy, drowsy, and dull" (influenza, mono, CFS...)
• Gelsemium patients also have Anticipatory anxiety with trembling, examination funk and Timidity in public, cowardice (diarrhea from fear).
• Better on closing eyes, bending forward (headache is better with profuse urination).
• Worse: in sun, heat, summer, damp weather, excitement, periodically.

Nutrition

• Too high intakesugar can have deleterious effects on immune function, especially in fighting bacterial infection.
• Pro-inflammatory protein levels can increase due to sugar intakes.
• Simple carbohydrates can decrease phagocytic capacity of neutrophils (last up to 5 hrs.)
• A deficiency in dietary protein/amino acids impairs immune function and increases susceptibility to infection.
• Honey has natural antimicrobial properties and used traditionally as antibiotic.
• Decreases inflammation and Symptomatic management by easing discomfort can occur.
• Probiotics safe and well-tolerated help Support healthy microbiome, especially antibiotic use.
• Consider intake when supporting, Streptococcus salivarius K12 (SsK12) may offer specific supper with strep throat infection
• Vitamin D has been shown to enhance neutrophil killing of pathogenic streptococcal bacteria, while dampening excessive inflammatory responses and apoptosis.
• Vitamin C supplementation (along with antiviral regimens provides increased effect.
• Vitamin C has efficacy and provides symptom amelioration support.
• Found to shorten duration of symptoms compared to placebo.
• Total efficacy, time for symptom amelioration, and time for healing were better.
• Found to shorten duration of symptoms compared to placebo
• More effective in adults than in children
• Bad taste and nausea were most common adverse effects

Measures Of Safety

• LD50 = dose at which causes death in 50% of individuals.
• ED50 = dose at which causes therapeutic response in 50% of individuals.
• Want range as far apart as possible.